Reference 06 08 2012 125652

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1. A facile synthesis and cytotoxicity of a novel porphyrin-cryptolepine conjugate By Kumar, Dalip; Shekar, K. P. Chandra; Mishra, Bhupendra; Kumar, Anil; Akamatsu, Kanako; Kusaka, Eriko; Ito, Takeo From Chemistry & Biology Interface (2012), 2(2), 114-121. Language: English, Database: CAPLUS
A novel porphyrin-cryptolepine conjugate 7 with a 1,2,3-triazole linker was synthesized by the cycloaddn. reaction of propargyl porphyrin 2 and azido cryptolepine 6 under click conditions. The conjugate 7 exhibited enhanced photocytotoxicity against A549 cells with IC50 values of 2.5 M and 7.9 M in the visible and UV light, resp. ~0 Citings
Copyright 2012 American Chemical Society (ACS). All Rights Reserved.
2. One-pot, three-component synthesis of 1-amidomethyl-imidazo[1,2-a]pyridines catalyzed by ytterbium triflate By Pericherla, Kasiviswanadharaju; Khungar, Bharti; Kumar, Anil From Tetrahedron Letters (2012), 53(10), 1253-1257. Language: English, Database: CAPLUS, DOI:10.1016/j.tetlet.2011.12.121
A straightforward method has been developed for the synthesis of 1-amidomethyl-imidazo[1,2-a]pyridines by Yb(OTf)3 catalyzed three-component reaction of aldehydes, acetamide, and imidazo[1,2-a]pyridines. A series of substituted 3substituted imidazo[1,2-a]pyridines were synthesized in moderate to good yield (21-74%) under mild reaction condition and the catalyst was recycled for four cycles. ~0 Citings
3. Analysis of surface and guided wave plasmon polariton modes in insulator-metal-insulator planar plasmonic waveguides By Sharma, V. K.; Kumar, Anil; Kapoor, A. From Optics Communications (2012), 285(6), 1123-1127. Language: English, Database: CAPLUS, DOI:10.1016/j.optcom.2011.10.070
Theor. and exptl. study of the surface plasmon-polariton and guided wave plasmon polariton modes is presented for the Sapphire/Ag/Polycarbonate/Air structure. Theor. results are obtained by solving complex multilayer eigenvalue equations as well as the reflectivity equation for this structure. It is proposed that the mode attenuation can be significantly reduced by inserting a low index dielec. buffer between the metal and the guiding dielec. layer. The dispersion and attenuation curves are generated. Both the surface plasmon and guided wave plasmon polariton modes are studied exptl. The exptl. values of the effective refractive indexes agree well with the theor. values. The elec. field profiles are generated and used to examine the nature of modes. After optimization of various parameters the condition for low loss single mode guiding is obtained for the proposed structure. Effect of metal thickness on
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surface plasmon mode is also discussed. It is inferred that in a properly optimized plasmonic waveguide, the losses can be reduced by a factor of 4. ~0 Citings
4. Microwave-assisted and scandium triflate catalyzed synthesis of tetrahydrobenzo[a]xanthen-11-ones By Rao, Madharam Sudershan; Chhikara, Bhupender S.; Tiwari, Rakesh; Shirazi, Amir N.; Parang, Keykavous; Kumar, Anil From Monatshefte fuer Chemie (2012), 143(2), 263-268. Language: English, Database: CAPLUS, DOI:10.1007/s00706-011-0577-4
Synthesis of 12-aryl-8,9,10,12-tetrahydro-benzo[a]xanthen-11-ones was achieved by one-pot condensation of naphthol, substituted benzaldehydes, and 1,3-dicarbonyl compds. catalyzed by Sc(OTf)3 under microwave irradn. in excellent isolated yields. The catalyst was recycled up to four cycles with no appreciable loss in catalytic activity. The compds. were evaluated for Src kinase activity and anticancer activity. ~1 Citing
5. One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their antiproliferative and Src kinase inhibitory activities By Rao, V. Kameshwara; Chhikara, Bhupender S.; Tiwari, Rakesh; Shirazi, Amir Nasrolahi; Parang, Keykavous; Kumar, Anil From Bioorganic & Medicinal Chemistry Letters (2012), 22(1), 410-414. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2011.10.124
EA no. of 2-substituted tetrahydroindazolones were synthesized by three-component condensation reaction of 1,3diketones, substituted hydrazines, benzaldehydes, and Yb(OTf)3 as a catalyst in [bmim][BF4] ionic liq. using a simple, efficient, and economical one-pot method. The synthesized tetrahydroindazolones were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. 3,4-Dichlorophenyl tetrahydroindazolone deriv. inhibited the cell proliferation of HT-29 and SK-OV-3 cells by 62% and 58%, resp. 2,3-Diphenyl-substituted tetrahydroindazolone derivs. inhibited the cell proliferation of HT-29 cells by 65-72% at a concn. of 50 M. In general, the tetrahydroindazolones showed modest inhibition of c-Src kinase where 4-tert-butylphenyl- and 3,4-dichlorophenyl- derivs. showed the inhibition of c-Src kinase with IC50 values of 35.1 and 50.7 M, resp. ~0 Citings
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6. Saccharide derived dinuclear Cu(II) complex: An efficient catalyst for oxidation of catechol and benzylic alcohols By Soni, Kiran; Kumar, Anil; Sah, Ajay K. From Catalysis Communications (2012), 17, 95-98. Language: English, Database: CAPLUS, DOI:10.1016/j.catcom.2011.10.018
Catalytical aspect of 4,6-O-ethylidene--D-glucopyranosylamine derived dinuclear Cu(II) complex has been explored. The complex exhibits good catecholase like activity and oxidizes model substrate 3,5-di-tert-butylcatechol to 3,5-ditert-butyl-o-quinone. The complex also acts as a selective catalyst to oxidize the primary and secondary alcs. to the corresponding carbonyl compds. in excellent yield (65-82%) under mild conditions. ~0 Citings
7. Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities By Rao, Vagicherla Kameshwara; Rao, Madharam Sudershan; Jain, Navin; Panwar, Jitendra; Kumar, Anil From Organic and Medicinal Chemistry Letters (2011), 1(1), 10, 7 pp.. Language: English, Database: CAPLUS, DOI:10.1186/2191-2858-1-10
An efficient, one-pot synthesis was developed and the synthesis of the target compds. was achieved by a threecomponent coupling reaction of aldehydes, N-methylaniline and indole derivs. using AgOTf as a catalyst. Several aminoalkyl indole derivs. [i.e., N-methyl-N,-diphenyl-1H-indole-3-methanamine derivs.] were evaluated for their antibacterial activity against both Gram-neg. and Gram-pos. bacteria. Two compds. displayed good antibacterial activity against both Gram-pos. and Gram-neg. strains. However, inversion of substituent properties resulted in a significant drop in magnitude of antibacterial activity against Escherichia coli. ~0 Citings
8. Ytterbium(III) triflate: An efficient and simple catalyst for isomerization of 2'-hydroxychalcone and 2'-aminochalcones in ionic liquid By Rao, V. Kameswara; Rao, M. Sudershan; Kumar, Anil From Journal of Heterocyclic Chemistry (2011), 48(6), 1356-1360. Language: English, Database: CAPLUS, DOI:10.1002/jhet.760
Isomerization of 2'-hydroxychalcone and 2'-aminochalcone have been investigated using ytterbium(III) trifluromethanesulfonate {Yb(OTf)3} (30 mol %) as Lewis acid catalyst in [bmim][BF4] ionic liq. The effect of different metal triflates as Lewis acid, catalyst loading, and reaction media was studied for this isomerization reaction. Advantages of the methodol. include short reaction time, excellent yields, catalytic use of Lewis acid, and recovery and reuse of the catalyst.
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9. Carbon dioxide (Co2) utilizing strain database By Saini, Rashmi; Majhi, Manash C.; Kapoor, Rupam; Kumar, Rita; Kumar, Anil From African Journal of Biotechnology (2011), 10(63), 13818-13822. Language: English, Database: CAPLUS
Culling of excess carbon dioxide from our environment is one of the major challenges to scientific communities. Many phys., chem. and biol. methods have been practiced to overcome this problem. The biol. means of CO2 fixation using various microorganisms is gaining importance because database of their substantial role in reversing global warming. Carbon dioxide utilizing strain database (CSD) presents a comprehensive overview of microorganisms involved in biol. fixation of carbon dioxide. As a part of this work, the wealth of information on CO2 utilizing strains was first collected and was then managed within four classes, i.e., microorganisms, genus listing, mechanisms and literature. The first two classes consolidate information regarding the microbial genus and species, while the later two provide information regarding the CO2 fixing pathways and the taxonomic details of these organisms. The database also holds the current information about the issue. CSD can be used to gain information related to CO2 fixing microbes. It can also contribute to devising biol. strategies for reducing carbon dioxide from the environment. It introduces an innovative idea of exploring the potential of these bacterial strains for reversing global warming. The CSD can be accessed online. ~0 Citings
10. Ionic Liquid-Supported Aldehyde: A Highly Efficient Scavenger for Primary Amines By Muthayala, Manoj Kumar; Kumar, Anil From ACS Combinatorial Science (2012), 14(1), 5-9. Language: English, Database: CAPLUS, DOI:10.1021/co200151n
Novel aldehyde-functionalized ionic liqs. have been synthesized and used as scavengers for primary amines in the synthesis of secondary amines. The yields of secondary amines are high (82-90%) with high purity. The advantages of the protocol over that with a polymersupported aldehyde scavenger are the shorter reaction time, the homogeneous reaction medium, the high level of loading of the aldehyde group, easy monitoring of reaction, and characterization of intermediates. ~0 Citings
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11. An efficient and simple synthesis of tetraketones catalyzed by Yb(OTf)3-SiO2 under solvent free conditions By Rao, V. Kameshwara; Kumar, Muthyala Manoj; Kumar, Anil From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2011), 50B(8), 11281135. Language: English, Database: CAPLUS
A novel and efficient 3-component 1-pot condensation method was described for the synthesis of tetraketones, i.e. arylmethylene-2,2'-bis(cyclohexane-1,3-diones) or arylmethylenebis(3-hydroxy-2-cyclohexen-1-ones), using Yb(O3SCF3)3-SiO2 and amine as catalytic system under solvent-free conditions. Tetraketones were obtained in high yield (73-88%). The application of an eco-friendly, non-corrosive, and reusable catalytic system makes this method advantageous. ~0 Citings
12. A simple and efficient bromoazidation of alkenes using PTT and TMSN3 in ionic liquid By Kumar, Anil; Rao, M. Sudershan; Mehta, Bibbor From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2011), 50B(8), 11231127. Language: English, Database: CAPLUS
A simple and efficient 1-pot method was described for the bromoazidation of alkenes using PhMe3NBr3 (PTT) and Me3SiN3 (TMSN3) in ionic liq. The bromo azides were obtained in good to excellent yield from various alkenes, such as styrenes, chalcones, and cycloalkenes, at room temp. ~0 Citings
13. Microwave-assisted and Yb(OTf)3-promoted one-pot multicomponent synthesis of substituted quinolines in ionic liquid By Kumar, Anil; Rao, V. Kameshwara From Synlett (2011), (15), 2157-2162. Language: English, Database: CAPLUS, DOI:10.1055/s-0030-1261200
A straightforward and efficient method has been developed for the synthesis of quinolines by Yb(OTf)3 catalyzed three-component reaction of aldehydes, alkynes, and amines under microwave irradn. in ionic liq. A series of 2,4disubstituted quinolines was synthesized in excellent yield (69-93%) under mild reaction condition and the catalyst was recycled for four cycles. ~1 Citing
14. A protic ionic liquid attenuates the deleterious actions of urea on -chymotrypsin By Attri, Pankaj; Venkatesu, Pannuru; Kumar, Anil; Byrne, Nolene From Physical Chemistry Chemical Physics (2011), 13(38), 17023-17026. Language: English, Database: CAPLUS, DOI:10.1039/c1cp22195g
We present a biocompatible ionic liq., tri-Et ammonium acetate (TEAA), that attenuates the denaturation action of a non-ionic chaotrope, urea, on the industrially relevant proteolytic enzyme -chymotrypsin. ~4 Citings
15. 1-Butyl-3-methylimidazolium p-toluenesulfinate: a novel reagent for synthesis of sulfones and -ketosulfones in ionic liquid By Kumar, Anil; Muthyala, Manoj Kumar From Tetrahedron Letters (2011), 52(41), 5368-5370. Language: English, Database: CAPLUS, DOI:10.1016/j.tetlet.2011.08.035
A novel task-specific ionic liq., 1-butyl-3-methylimidazolium p-toluenesulfinate, [bmim][p-TolSO2] has been synthesized and used as a nucleophile for the reaction with alkyl bromides and phenacyl bromides to prep. sulfones e. g., I and -ketosulfones e. g., II in excellent yields (80-93%) in [bmim][BF4] ionic liq. The isolated yields of sulfones and -ketosulfones were higher in [bmim][BF4] than other org. solvents at room temp.
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16. Cu(OTf)2 catalyzed synthesis of bis(5-methyl-2-furyl)methanes by condensation of 2-methylfuran with carbonyl compounds under solvent free conditions By Muthyala, Manoj Kumar; Rao, V. Kameswara; Kumar, Anil From Chinese Journal of Chemistry (2011), 29(7), 1483-1488. Language: English, Database: CAPLUS, DOI:10.1002/cjoc.201180269
A facile and efficient 1-pot 3-component synthesis of bis(5-methyl-2-furyl)methanes was achieved via the reaction of 2-methylfuran with a series of aliph. and arom. aldehydes and aliph. ketones in the presence of Cu(II) triflate under solvent-free conditions. The bis(5-methyl-2-furyl)methanes were obtained in 34-72% yields, and the catalyst was recycled 4 successive cycles without much loss in catalytic activity. ~0 Citings
17. 3-Substituted indoles: one-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities By Rao, V. Kameshwara; Chhikara, Bhupender S.; Shirazi, Amir Nasrolahi; Tiwari, Rakesh; Parang, Keykavous; Kumar, Anil From Bioorganic & Medicinal Chemistry Letters (2011), 21(12), 3511-3514. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2011.05.010
An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot threecomponent coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or Nmethylindole using Yb(OTf)3-SiO2 as a catalyst. All the synthesized compds. were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. Compds. I (R = OMe, R' = 4-MePh; R = Br, R' = 4-MePh; R = Br, R' = 4-OMePh) inhibited the cell proliferation of SK-OV-3 and HT-29 cells by 70-77% at a concn. of 50 M. Compds. I (R = H, R' = Ph; R = H, R' = 3-NO2Ph) showed the inhibition of c-Src kinase with IC50 values of 50.6 and 58.3 M, resp.
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~7 Citings
18. Fatty acyl amide derivatives of doxorubicin: Synthesis and in vitro anticancer activities By Chhikara, Bhupender S.; St. Jean, Nicole; Mandal, Deendayal; Kumar, Anil; Parang, Keykavous From European Journal of Medicinal Chemistry (2011), 46(6), 2037-2042. Language: English, Database: CAPLUS, DOI:10.1016/j.ejmech.2011.02.056
Doxorubicin is extensively used in anticancer therapy. Doxorubicin is highly hydrophilic, has short half-life, and its use is assocd. with severe side effects at high doses. Fatty acyl amide derivs. of doxorubicin were synthesized with the expectation to improve the lipophilicity and anticancer activity of the drug. The lipophilicity was enhanced with the increase in chain length of fatty acyl moiety. Conjugation of 4'-amino group with fatty acids through an amide bond reduced the anticancer activity in leukemia, breast, ovarian, and colon cancer cell lines, suggesting that the presence of free amino group is required for anticancer activity of doxorubicin. Dodecanoyl-doxorubicin deriv. was consistently the most effective among the synthesized derivs. and inhibited the proliferation of colon (HT-29) and ovarian (SK-OV3) cancer cells by 64% and 58%, resp., at a concn. of 1 M after 96 h incubation. ~3 Citings
19. Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities By Kumar, Anil; Ahmad, Israr; Chhikara, Bhupender S.; Tiwari, Rakesh; Mandal, Deendayal; Parang, Keykavous From Bioorganic & Medicinal Chemistry Letters (2011), 21(5), 1342-1346. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2011.01.047
A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chem. approach. All compds. were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 M. 4-Methoxyphenyl triazolylsubstituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, resp., at a concn. of 50 M. ~7 Citings
20. High extinction ratio metal-insulator-semiconductor waveguide surface plasmon polariton polarizer By Sharma, V. K.; Kumar, Anil; Kapoor, A. From Optics Communications (2011), 284(7), 1815-1821. Language: English, Database: CAPLUS,
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DOI:10.1016/j.optcom.2010.11.079
The attenuation characteristics of a multilayer metal clad GaAs-AlGaAs optical waveguide polarizer are theor. investigated. The dispersion relations and field distribution of the multilayer structures are calcd. for different geometrical parameters and material properties. The polarizer studied consists of a single mode finite/infinite metal clad GaAs-AlGaAs waveguide with a dielec. (SiO2/Si3N4) buffer layer inserted between the metal and the waveguide.Conventionally, the TM polarized waves are found to exhibit an absorption peak at a particular buffer thickness (called crit. buffer thickness).We shall show that the max. TM absorption can be improved by a multiple factor up to 7 by choosing a buffer layer thicker than its crit. value. This corresponds to an extinction ratio of 1470 dB for a polarizer length of 1 mm. Further, thicker buffers reduce the insertion losses and values as low as 0.1 dB can be obtained. The strong TM absorption in these structures is interpreted as resonant coupling of the guided mode to the lossy surface plasmon polariton supported by the thin metal film. Thicker buffer also reduces the TE losses (insertion losses) and hence increases the extinction ratio (ratio of TM to TE losses).This can be achieved by optimizing the buffer and the metal thicknesses. Another equally efficient polarizer can be designed by positioning a dielec. (same as buffer) layer (superstrate layer) above the metal film and then optimizing the buffer, metal and the superstrate thicknesses. We also show that the proposed polarizer with the superstrate layer is highly stable even when exposed to the extreme atm. changes. ~3 Citings
21. Synthesis and fluorescence studies of porphyrin appended 1,3,4-oxadiazoles By Chandra Shekar, K. P.; Mishra, Bhupendra; Kumar, Anil; Phukan, S.; Mitra, S.; Kumar, Dalip From Journal of Porphyrins and Phthalocyanines (2010), 14(12), 1034-1039. Language: English, Database: CAPLUS, DOI:10.1142/S1088424610002884
A modular synthetic approach for prepg. a family of tetraarylporphyrin 1,3,4-oxadiazole derivs. I [R = Ph, C6H4-4-Me, -4-OMe, -4-Cl, -4-NO2, 4-pyridyl] was described. A corresponding porphyrin hydrazide was reacted with aryl aldehydes in presence of Yb(OTf)3 as catalyst to give intermediate porphyrin hydrazones which were then cyclized using iodobenzene diacetate to give the desired conjugates. Photophys. studies in CHCl3 solvent shows that the electronic structure of the porphyrin chromophore is not greatly perturbed by the incorporation of the oxadiazole group onto the meso-Ph ring. Efficient quenching of porphyrin fluorescence was obsd. in I [R = 1-methyl-4-pyridinium iodide].
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22. Activity and stability of -chymotrypsin in biocompatible ionic liquids: enzyme refolding by triethyl ammonium acetate By Attri, Pankaj; Venkatesu, Pannuru; Kumar, Anil From Physical Chemistry Chemical Physics (2011), 13(7), 2788-2796. Language: English, Database: CAPLUS, DOI:10.1039/c0cp01291b
In view the of wide scope of structural information of biomols. in biocompatible ionic liqs. (ILs) in various applications including chem. and biochem., it is essential to study the productive preferential interactions between biol. macromols. and biocompatible ILs. The authors have therefore explored the stability and activity of -chymotrypsin (CT) in the presence of five ILs from different families, such as tri-Et ammonium acetate (TEAA), tri-Et ammonium phosphate (TEAP) from ammonium salts, 1-benzyl-3-methylimidazolium chloride ([Bzmim][Cl]), 1-benzyl-3-methylimidazolium tetrafluoroborate ([Bzmim][BF4]) from imidazolium salts and tetra-Bu phosphonium bromide (TBPBr) from phosphonium families. CD and UV-visible spectrophotometer expts. were used to study CT stabilization by ILs, related to the assocd. structural changes and enzyme activity studies, resp. All ILs have a dominant contribution to the stabilization of CT. The stability and activity of CT depends on the structural arrangement of the ions of ILs. The authors' exptl. results explicitly elucidate that more hydrophobic imidazolium and phosphonium cations carrying longer alkyl chains of ILs ([Bzmim][Cl], [Bzmim][BF4] and TBPBr) were weak stabilizers for CT, while small alkyl chain mols. of tri-Et ammonium salts (TEAA and TEAP) are strong stabilizers and therefore more biocompatible for CT stability. The authors' CD and NMR measurements reveal that TEAA is a refolding additive for CT from a quenched thermal unfolded enzyme structure. ~13 Citings
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23. Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity By Kumar, Dalip; Reddy, V. Buchi; Kumar, Anil; Mandal, Deendayal; Tiwari, Rakesh; Parang, Keykavous From Bioorganic & Medicinal Chemistry Letters (2011), 21(1), 449-452. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2010.10.121
Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of -tosyloxy ketones/-halo ketones, sodium azide, and terminal alkynes in the presence of aq PEG (1:1, vol./vol.) using the click chem. approach and evaluated for Src kinase inhibitory activity. Structure-activity relationship anal. demonstrated that insertion of C6H5- and 4-CH3C6H4- at position 4 for both classes and less bulkier arom. group at position 1 in class 1 contribute critically to the modest Src inhibition activity (IC50 = 32-43 M) of 1,4-disubstituted 1,2,3-triazoles. ~9 Citings
24. A novel and short synthesis of naturally occurring 5-(3'-indolyl)oxazoles By Kumar, Dalip; Sundaree, Swapna; Petel, Gautam; Kumar, Anil From Journal of Heterocyclic Chemistry (2010), 47(6), 1425-1428. Language: English, Database: CAPLUS, DOI:10.1002/jhet.472
A novel, concise, and convenient synthesis of 5-(3'-indolyl)oxazoles by cyclization of 3-acetylindole with nitriles using the relatively benign reagent [hydroxy(2,4-dinitrobenzenesulfonyloxy)iodo]benzene was described. The advantages of this procedure include operational simplicity, good yield, and avoidance of toxic metal. ~1 Citing
25. Sodium Dodecyl Sulfate-assisted Synthesis of 1-(Benzothiazolylamino)methyl-2-naphthols in Water By Kumar, Anil; Rao, M. Sudershan; Rao, V. Kameswara From Australian Journal of Chemistry (2010), 63(11), 1538-1540. Language: English, Database: CAPLUS, DOI:10.1071/CH10209
An efficient synthesis of 1-[(benzothiazolylamino)(aryl)methyl]-2-naphthols has been developed in water by one-pot condensation of 2-naphthols, aldehydes and 2-aminobenzothiazole catalyzed by sodium dodecyl sulfate. Advantages of the methodol. include a very short reaction time, excellent yields and catalytic use of the sodium dodecyl sulfate. ~4 Citings
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26. Synthesis, antiviral and contraceptive activities of nucleoside-sodium cellulose sulfate acetate and succinate conjugates By Agarwal, Hitesh K.; Kumar, Anil; Doncel, Gustavo F.; Parang, Keykavous From Bioorganic & Medicinal Chemistry Letters (2010), 20(23), 6993-6997. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2010.09.133
Chem. conjugates between sodium cellulose sulfate (CS), displaying contraceptive and HIV-entry inhibiting properties, and nucleoside reverse transcriptase inhibitors (NRTIs) (3'-azido-2',3'-dideoxythymidine (AZT), 3'-fluoro-2',3'dideoxythymidine (FLT), or 2',3'-dideoxy-3'-thiacytidine (3TC)) were designed to simultaneously provide contraceptive and anti-HIV activity. Two linkers, acetate and succinate, were used to conjugate the nucleoside analogs with CS. The conjugates contg. cellulose sulfate-acetate (CSA) (e.g., AZT-CSA and FLT-CSA) were more potent than CS and other conjugates (e.g., AZT-succinate-CS, and FLT-succinate-CS). The presence of both sulfate and the acetate groups on cellulose were crit. for generating max. anti-HIV activity. In addn. to showing equal potency against wildtype and multidrug resistant HIV-1, the AZT-CSA conjugate displayed significant contraceptive activity in an animal model, providing the initial proof-of-concept for the design and synthesis of dual-activity compds. based on these combinations. ~4 Citings
27. Temperature Effect on the Molecular Interactions between Ammonium Ionic Liquids and N,N-Dimethylformamide By Attri, Pankaj; Venkatesu, Pannuru; Kumar, Anil From Journal of Physical Chemistry B (2010), 114(42), 13415-13425. Language: English, Database: CAPLUS, DOI:10.1021/jp108003x
In view of the wide scope of mol. interactions between the highly polar compd. of N,N-dimethylformamide (DMF) and ammonium ionic liqs. (ILs), we have measured thermophys. properties such as densities () and ultrasonic sound velocities (u) over the whole compn. range at temps. ranging from 25 to 50 C under atm. pressure. To gain some insight into the several aggregations of mol. interactions present in these mixed solvents, we predicted the excess molar volume (VE) and the deviations in isentropic compressibilities (Ks) as a function of the concn. of IL. These results are fitted to the Redlich-Kister polynomials. The materials investigated in the present study included the hydroxide series of ammonium ILs of tetramethylammonium hydroxide [(CH3)4N][OH] (TMAH), tetraethylammonium hydroxide [(C2H5)4N][OH] (TEAH), and tetrapropylammonium hydroxide [(C2H7)4N][OH] (TPAH). The intermol.
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interactions and structural effects were analyzed on the basis of the measured and the derived properties. A qual. anal. of the results is discussed in terms of the ion-dipole and ion-pair interactions, and hydrogen bonding between ILs and DMF mols. and their structural factors. ~11 Citings
28. Measurements and Molecular Interactions for N,N-Dimethylformamide with Ionic Liquid Mixed Solvents By Attri, Pankaj; Reddy, P. Madhusudan; Venkatesu, P.; Kumar, Anil; Hofman, T. From Journal of Physical Chemistry B (2010), 114(18), 6126-6133. Language: English, Database: CAPLUS, DOI:10.1021/jp101209j
To understand the mol. interactions between N,Ndimethylformamide (DMF) with two families of ionic liqs. (ILs), we have measured thermophys. properties such as densities () and ultrasonic sound velocities (u) over the whole compn. range at 25 C under atm. pressure. The excess molar volume (VE) and the deviation in isentropic compressibilities (Ks) were predicted using these properties as a function of the concn. of IL. These results are fitted to the Redlich-Kister polynomials. The materials investigated in the present study included two families of ILs such as ammonium salts and imidazolium salts. Diethylammonium acetate ([Et2NH][CH3COO], DEAA), triethylammonium acetate ([Et3NH][CH3COO], TEAA), triethylammonium dihydrogen phosphate ([Et3NH] [H2PO4], TEAP), and triethylammonium sulfate ([Et3NH] [HSO4], TEAS) are ammonium salts and 1-benzyl-3methylimidazolium chloride ([Bmim][Cl]) belongs to the imidazolium family. The intermol. interactions and structural effects were analyzed on the basis of the measured and the derived properties. A qual. anal. of the results is discussed in terms of the ion-dipole, ion-pair interactions, and hydrogen bonding between ILs and DMF mols. and their structural factors. ~15 Citings
29. Cerium triflate: an efficient and recyclable catalyst for chemoselective thioacetalization of carbonyl compounds
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under solvent-free conditions By Kumar, Anil; Rao, M. Sudershan; Kameshwara Rao, V. From Australian Journal of Chemistry (2010), 63(1), 135-140. Language: English, Database: CAPLUS, DOI:10.1071/CH09296
A simple and efficient chemoselective thioacetalization of carbonyl compds. was achieved using Ce(OTf)3 (10 mol%) as a catalyst under solvent-free conditions. Advantages of the methodol. include very short reaction times, excellent yields, the catalytic use of a water-tolerant Lewis acid, and simple recovery and reuse of the catalyst. ~10 Citings
30. Algorithmic technique for decomposing unitary operations in NMR quantum computation By Ajoy, Ashok; Samal, Jharna Rani; Kumar, Anil From arXiv.org, e-Print Archive, Quantum Physics (2009), 1-14, arXiv:0911.5467v1 [quant-ph]. Language: English, Database: CAPLUS
We present an algorithmic technique for decompg. unitary operations in NMR quantum computation. Possible applications in simulating Hamiltonians in NMR; and obtaining pulse sequences in constrainted systems - like the Ising spin chain with nearest neighbor interactions are suggested. NMR pulse sequences for several N-bit quantum gates: the Toffoli, Fredkin, 2, Fanout, Parity, and SWAP gates are developed. Pulse sequences for the Toffoli, Fredkin and 2 gates scale exponentially with the no. of qubits. Pulse sequences for Fanout, Parity, and SWAP gates scale polynomially and these gates can be implemented efficiently on Ising spin chains. ~0 Citings
31. A simple and efficient thia-Michael addition to ,-unsaturated ketones catalyzed by Yb(OTf)3 in [bmim][BF4] By Kumar, Anil; Ahmad, Israr; Sudershan Rao, M. From Journal of Sulfur Chemistry (2009), 30(6), 570-577. Language: English, Database: CAPLUS, DOI:10.1080/17415990903281041
Yb(OTf)3 in an ionic liq. [bmim][BF4] is reported as an efficient catalyst for the thia-Michael addn. of thiols to ,unsatd. ketones to give -aryl--mercapto ketones in 82-94% yield and the catalyst along with ionic liq. was recycled and reused. ~9 Citings
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32. Ionic liquid catalyzed expeditious synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones and 2-aryl-2,3-dihydro-4Hchromen-4-ones under microwave irradiation By Kumar, Dalip; Patel, Gautam; Kumar, Anil; Roy, Ram K. From Journal of Heterocyclic Chemistry (2009), 46(4), 791-795. Language: English, Database: CAPLUS, DOI:10.1002/jhet.123
A facile and convenient synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones and -4H-chromen-4-ones was described using ionic liq.-catalyzed intramol. cyclization of the corresponding 2'-amino- and 2'-hydroxychalcones, resp. The rapid and fairly general protocol affords the products in good yield. The ionic liq., 1-butyl-3-methylimidazolium tetrafluoroborate, was recovered and reused without loosing its efficiency. ~5 Citings
33. A simple and efficient PTT-mediated synthesis of -azidoketones in [bmim][BF4] ionic liquid By Kumar, Anil; Ahmed, Israr; Rao, M. Sudershan; Patel, Gautam; Kumar, Dalip From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2009), 48B(4), 611616. Language: English, Database: CAPLUS
A simple and efficient one-pot method has been described for the direct synthesis of -azidoketones in high yields from various ketones possessing -hydrogen via the reaction with phenyltrimethylammonium tribromide followed by the reaction with NaN3 in ionic liq. ~7 Citings
34. A simple and facile synthesis of amidoalkyl naphthols catalyzed by Yb(OTf)3 in ionic liquids By Kumar, Anil; Rao, M. Sudershan; Ahmad, Israr; Khungar, Bharti From Canadian Journal of Chemistry (2009), 87(6), 714-719. Language: English, Database: CAPLUS, DOI:10.1139/V09-049
An improved, simple, and facile synthesis of amidoalkyl naphthols by employing three-component one-pot condensation reaction of -naphthol, arom. aldehydes, and amides in ionic liqs. using ytterbium triflate as a mild Lewis acid catalyst is described. Advantageously, amidoalkyl naphthols were obtained in high yield under eco-friendly, economical, and non-corrosive conditions, and the catalyst was recycled. ~13 Citings
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35. An efficient and simple one-pot synthesis of -acetamido ketones catalyzed by ytterbium triflate in ionic liquid By Kumar, Anil; Rao, M. Sudershan; Ahmad, Israr; Khungar, Bharti From Australian Journal of Chemistry (2009), 62(4), 322-327. Language: English, Database: CAPLUS, DOI:10.1071/CH08557
Ytterbium triflate immobilized in the ionic liq. [bmim][BF4] catalyzes the three-component coupling of arom. aldehydes, enolizable ketones, and acetonitrile in the presence of acetyl chloride at room temp. to afford -acetamido ketones in good yields. The catalyst can be recovered and recycled for subsequent reactions without any appreciable loss of efficiency. ~12 Citings
36. Ytterbium(III) triflate catalyzed synthesis of calix[4]pyrroles in ionic liquids By Kumar, Anil; Ahmad, Israr; Rao, M. Sudershan From Canadian Journal of Chemistry (2008), 86(9), 899-902. Language: English, Database: CAPLUS, DOI:10.1139/V08-121
Ytterbium(III) triflate was used as a mild Lewis acid catalyst for the synthesis of calix[4]pyrroles by the condensation of pyrrole with different ketones in ionic liqs. The calix[4]pyrroles were obtained in high yield under eco-friendly, economical, and noncorrosive conditions, and the catalyst was recovered and recycled. ~16 Citings
37. Synthesis of cellulose sulfate-nucleoside conjugates as bifunctional anti-HIV agents By Agarwal, Hitesh Kumar; Kumar, Anil; Doncel, Gustavo F.; Parang, Keykavous From Abstracts of Papers, 236th ACS National Meeting, Philadelphia, PA, United States, August 17-21, 2008 (2008), MEDI-442. Language: English, Database: CAPLUS
Sodium cellulose sulfate has been introduced as an inhibitor of HIV entry and sperm-function. Bifunctional conjugates contg. sodium cellulose sulfate and anti-HIV nucleoside reverse transcriptase inhibitors (AZT, FLT, and 3TC) were synthesized using different linkers to obtain synergistic activity. Three linkers, succinate, acetyl, and glutamate, were used to conjugate the nucleosides with the polymer. Nucleosides (AZT and FLT) were reacted with succinic anhydride to make nucleoside succinate building blocks. Nucleoside succinates were then reacted with the polymer in presence of DIC as a coupling reagent to give KPH-4ASC and KPH-4FSC. When acetyl group was used as a linker, sodium cellulose sulfate was first reacted with 2-bromoacetic acid to make modified cellulose sulfate that was reacted with AZT, FLT, and 3TC to give KPH-4ACA, KPH-4FCA, and KPH-43CA, resp. Finally, FLT was reacted with FmocGlu-O tBu. Deprotection of tert-Bu followed by the reaction with sodium cellulose sulfate in the presence of DIC
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afforded KPH-43GC. ~0 Citings

38. Synthesis and evaluation of 3-phenylpyrazolo[3,4-d]pyrimidine-peptide conjugates as Src kinase inhibitors By Kumar, Anil; Wang, Yuehao; Lin, Xiaofeng; Sun, Gongqin; Parang, Keykavous From ChemMedChem (2007), 2(9), 1346-1360. Language: English, Database: CAPLUS, DOI:10.1002/cmdc.200700074
3-Phenylpyrazolo[3,4-d]pyrimidine (PhPP) derivs. substituted with an alkyl or aryl carboxylic acid at the N1-endocyclic amine, such as PhPP-CH2COOH (IC50 = 250 M), and peptides Ac-CIYKYY (IC50 = 400 M) and Ac-YIYGSFK (IC50 = 570 M) were weak inhibitors of polyE4Y phosphorylation by active c-Src. A series of PhPP-peptide conjugates were synthesized using PhPP as an ATP mimic and CIYKYY or YIYGSFK as a peptide substrate to improve the inhibitory potency against active c-Src kinase. PhPP derivs. were attached to the N-terminus or the side chain of amino acids in the peptide template. Two N-terminal substituted conjugates, PhPP-CH2CO-CIYKYY (IC50 = 0.38 M) and PhPP-CH2CO-YIYGSFK (IC50 = 2.7 M), inhibited the polyE4Y phosphorylation by active c-Src significantly higher than that of the parent compds. The conjugation of PhPP with the peptides produced a synergistic inhibition effect possibly through creation of favorable interactions between the conjugate and the kinase domain as shown by mol. modeling studies. ~13 Citings
39. Noncovalent cellular delivery of phosphopeptides by amphipathic peptides By Ye, Guofeng; Nam, Nguyen H.; Kumar, Anil; Parang, Keykavous From Abstracts of Papers, 234th ACS National Meeting, Boston, MA, United States, August 19-23, 2007 (2007), MEDI-112. Language: English, Database: CAPLUS
A no. of amphipathic peptides contg. two arginine and one lysine residues were synthesized and evaluated for noncovalent cellular delivery of phosphopeptides. Fluorescence polarization assay showed that peptides contg. long hydrophobic linkers, such as LPA4, can form a complex with the fluorescein-labeled GpYEEI (F-GpYEEI). LPA4 was further evaluated for potential application in cellular delivery of phosphopeptides to BT-20 live cells. Confocal microscopy and fluorescent flow cytometry studies with the mixt. of LPA4 (50 M) and F-GpYEEI (10 M) in BT-20 cells showed dramatic increase in the fluorescence intensity in cytosol of cells after 30 min, suggesting that LPA4 can function as a delivery tool of F-GpYEEI. LPA1 was used as a neg. control. LPA4 was not able to deliver other control peptides, F-AMpYSSV and F-GpYTKM, into the cells. These studies suggest that pos.-charged amphipathic peptides can be used for non-covalent cellular delivery of specific phosphopeptides, and confirm our earlier results in the fixed cells. ~0 Citings
40. Synthesis and Evaluation of Tripodal Peptide Analogues for Cellular Delivery of Phosphopeptides By Ye, Guofeng; Nam, Nguyen-Hai; Kumar, Anil; Saleh, Ali; Shenoy, Dinesh B.; Amiji, Mansoor M.; Lin, Xiaofeng; Sun, Gongqin; Parang, Keykavous From Journal of Medicinal Chemistry (2007), 50(15), 3604-3617. Language: English, Database: CAPLUS, DOI:10.1021/jm070416o
Tripodal peptide analogs were designed on the basis of the phosphotyrosine binding pocket of the Src SH2 domain and assayed for their ability to bind to fluorescein-labeled phosphopeptides. Fluorescence polarization assays showed that a no. of amphipathic linear peptide analogs (LPAs), such as LPA4 [H-Lys-NH(CH2)11CO-ArgNH(CH2)11CO-Arg-OH] , bind to fluorescein-labeled GpYEEI (F-GpYEEI; F = 5-carboxyfluorescein, G = Gly, pY = phosphotyrosine, E = Glu, I = Ile). LPA4 was evaluated for potential application in cellular delivery of phosphopeptides. Fluorescence microimaging cellular uptake studies with fluorescein-attached LPA4 (F-LPA4) alone or with the mixt. of LPA4 and F-GpYEEI in BT-20 cells showed dramatic increase of the fluorescence intensity in cytosol of cells, indicating that LPA4 can function as a delivery tool of F-GpYEEI across the cell membrane. Fluorescent flow cytometry studies showed the cellular uptake of F-LPA4 in an energy-independent pathway and confirmed the cellular uptake of F-GpYEEI in the presence of LPA4. These studies suggest that amphipathic tripodal peptide analogs, such as LPA4, can be used for cellular delivery of phosphopeptides. ~7 Citings
41. Epoxidation of alkenes with hydrogen peroxide catalyzed by 1-methyl-3-butylimidazoliumdecatungstate in ionic liquid By Kumar, Anil From Catalysis Communications (2007), 8(6), 913-916. Language: English, Database: CAPLUS, DOI:10.1016/j.catcom.2006.08.052
The epoxidn. of alkenes with hydrogen peroxide catalyzed by a new tungsten catalyst 1-methyl-3-
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butylimidazoliumdecatungstate in [bmim][BF4] ionic liq. was described. The epoxides were obtained in high yield, catalyst was recycled and the reaction conditions were simple and environmentally benign. ~9 Citings
42. Synthesis of nucleoside-succinate-dextran conjugates By Agarwal, Hitesh Kumar; Kumar, Anil; Mehvar, Reza; Parang, Keykavous From Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007 (2007), CARB-094. Language: English, Database: CAPLUS
Nucleoside-succinate-dextran conjugates were synthesized as the prodrugs of antiviral agents. Anti-HIV agents, zidouvudine, alovudine, and lamivudine, were subjected to reactions with succinic anhydride in the presence of N,Ndiisopropylethylamine to afford the corresponding 5'-O-succinate ester conjugates of nucleosides. Lamivudine was initially reacted with tert-butyldimethylsilyl chloride (TBDMS-Cl) in the presence of imidazole to yield 5'-O-TBDMSlamivudine. The protection of N4-amino group of 5'-O-protected lamivudine was carried out in the presence of 4,4'dimethoxytrityl chloride (DMTr-Cl) and pyridine to give N4-DMTr-5'-O-TBDMS-lamivudine. The deprotection of 5'-OTBDMS in the presence of tetrabutylammonium fluoride afforded N-4-DMTr deriv. of lamivudine, which was used in the reaction with succinyl anhydride to generate the lamivudine-succinate conjugate. 5'-O-Succinate ester conjugate of nucleosides were reacted with dextran (25 KD) in the presence of 1,3-diisopropylcarbodiimide and 4dimethylaminopyridine or triphenylphosphine and diisopropyl azodicarboxylate to afford the nucleoside-succinatedextran conjugates. N4-(DMTr)lamivudine-succinate-dextran conjugate was deprotected in the presence of acetic acid. The conjugates are expected to hydrolyze in vivo, resulting in sustained release of the parent nucleosides. ~0 Citings
43. Synthesis of methylprednisolone-peptide-dextran conjugates By Kumar, Anil; Nam, Nguyen H.; Agarwal, Hitesh Kumar; Mehvar, Reza; Parang, Keykavous From Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, March 25-29, 2007 (2007), CARB-093. Language: English, Database: CAPLUS
Dextran prodrugs of methylprednisolone (MP) contg. various peptide linkers were synthesized to evaluate the effects of linkers on the regeneration kinetics of MP in vitro. In general, all peptides were assembled on Fmoc-Gly-Wang resin or Wang resin by the solid-phase synthesis strategy employing Fmoc-based chem. and Fmoc-L-amino acid building blocks (i.e., Fmoc-Gly-OH, Fmoc-Sar-OH, or Fmoc-Phe-OH). 2-(1H-Benzotriazole-1-yl)-1,1,3,3tetramethyluronium hexafluorophosphate and N-methylmorpholine in N,N-dimethylformamide were used as coupling and activating reagents, resp. After the Fmoc deprotection with piperidine, the free N-terminal of the peptides was conjugated with 6--methylprednisolone succinate (MPS) to afford polymer-bound MPS-peptide conjugates. Acidic cleavage of the conjugates from Wang resin, followed by reaction with dextran (25 KD) in the presence of diisopropylcarbodiimide and 4-dimethylaminopyridine afforded MPS-peptide-dextran conjugates with approx. 8-9%
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loading values. Optimized dextran prodrugs of MP are expected to gradually regenerate the active drug in vivo, resulting in sustained immunosuppression in transplantation. We acknowledge the financial support from NIH (1 R01 GM069869-01A2). ~0 Citings
44. Biomimetic oxidation of veratryl alcohol with H2O2 catalyzed by iron(III) porphyrins and horseradish peroxidase in ionic liquid By Kumar, Anil; Jain, Nidhi; Chauhan, S. M. S. From Synlett (2007), (3), 411-414. Language: English, Database: CAPLUS, DOI:10.1055/s-2007-967951
3,4-Dimethoxybenzyl alc. (veratryl alc.) is a model compd. for lignin substructures and its oxidn. with H2O2 catalyzed by iron(III) porphyrins and horseradish peroxidase (HRP) in ionic liqs. is described. Veratraldehyde and 2hydroxymethyl-5-methoxy-2,5-cyclohexadiene-1,4-dione were the two major products of the oxidn. of veratryl alc. at room temp. The iron(III) porphyrin or HRP immobilized in ionic liqs. showed increased catalytic activity and can be recycled and this is believed due to the stabilization of high-valent oxoiron(IV) -cation radical intermediate generated in the reaction. ~26 Citings
45. Design and Evaluation of Hydroxamate Derivatives as Metal-Mediated Inhibitors of a Protein Tyrosine Kinase By Gu, Xianfeng; Wang, Yuehao; Kumar, Anil; Ye, Guofeng; Parang, Keykavous; Sun, Gongqin From Journal of Medicinal Chemistry (2006), 49(25), 7532-7539. Language: English, Database: CAPLUS, DOI:10.1021/jm061058c
Protein tyrosine kinases use two Mg2+ ions as cofactors in catalysis, one as the ATP-Mg complex (M1) and the other as an essential activator (M2). The M2-binding site has high affinity for transition metal cations such as cobalt and zinc. Taking advantage of this high affinity, we examd. hydroxamates as metal-mediated inhibitors against Cterminal Src kinase (Csk), a protein tyrosine kinase. Of a small group of amino acid hydroxamates, tyrosine and phenylalanine hydroxamates inhibited Csk activity only in the presence of Co2+. Four classes of phenylalanine and tyrosine hydroxamate derivs. were synthesized and evaluated as metal-mediated inhibitors of Csk, leading to improved inhibition and a better understanding of the structure-activity relationships. This study suggests that
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hydroxamates may serve as a general scaffold for developing metal-mediated inhibitors against protein tyrosine kinases. To the best of our knowledge, this is the first report of designing metal-mediated inhibitors against a protein tyrosine kinase by targeting a metal binding site. ~5 Citings
46. Application of two safety-catch linkers in solid-phase synthesis of sulfonamides By Kumar, Anil; Ye, Guofeng; Parang, Keykavous From Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006 (2006), ORGN-221. Language: English, Database: CAPLUS
Sulfonamides are currently used as therapeutic agents. Several solid-phase routes have been reported for the synthesis of sulfonamides. Unfortunately, for the synthesis of sulfonamides, polymer-bound reagents attached to safety-catch linkers have not been developed extensively. Two novel safety-catch linkers were synthesized by reaction between 4-(5'-formyl-2'-hydroxyphenyl)benzoic acid (1a) and 4-(5'-formyl-2'-hydroxyphenyl)phenyl propionic acid (1b), resp., with aminomethyl polystyrene resin (2) in the presence of 1-hydroxybenzotriazole and 1,3diisopropylcarbodiimide to afford 3. The phenolic hydroxyl group in 3 was acetylated by acetic anhydride. The reductive amination of a polymer-bound aldehyde 4 by amines (e.g., 4-chloroaniline, benzyl amine, 4-methoxybenzyl amine, aniline, 4-chloroaniline) and sodium triacetoxyborohydride gave 5. Sulfonylation of resin-bound amine 5 with alkyl or arylsulfonyl chloride derivs. in the presence of base afforded the polymer-bound sulfonamides 6. The cleavage of resin 6 in TFA/DCM produced the desired pure sulfonamides (7, overall yield 80-85%). ~0 Citings
47. Cellular delivery of phosphopeptides by positively-charged tripodal peptides By Ye, Guofeng; Nam, Nguyen H.; Kumar, Anil; Parang, Keykavous From Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006 (2006), MEDI-561. Language: English, Database: CAPLUS
Phosphopeptides are potenital inhibitors of interactions between phosphoproteins and pos.-charged amino acids in the binding pocket of enzymes involved in signal transduction pathways. However, the cellular delivery of neg.charged phosphopeptides is a difficult task. Tripodal pos.-charged peptides contg. two Arg and one Lys residues (11 compds.) were synthesized. The binding of peptides to phosphopeptide probes, such as fluorescein-attached phosphopeptide F-GpYEEI, was evaluated using a FP assay. Flow cytometry cellular uptake studies of F-GpYEEI were carried out by using human breast cancer cell lines, tripodal peptides (LPA-4 and LPA-1), and F-GYEEI as a neg. control. The mixt. of LPA-4 and F-GpYEEI exhibited a significantly higher mean fluorescence compared to that of F-GpYEEI alone and F-GpYEEI + LPA-1. F-GYEEI showed no uptake in the presence of LPA-1 and LPA-4. These
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data suggest that LPA-4 can function as delivery tool of neg.-charged F-GpYEEI across the cell membrane by specific interactions with the phosphate group. ~0 Citings
48. Synthesis and Structure-Activity Relationships of Linear and Conformationally Constrained Peptide Analogues of CIYKYY as Src Tyrosine Kinase Inhibitors By Kumar, Anil; Ye, Guofeng; Wang, Yuehao; Lin, Xiaofeng; Sun, Gongqin; Parang, Keykavous From Journal of Medicinal Chemistry (2006), 49(11), 3395-3401. Language: English, Database: CAPLUS, DOI:10.1021/jm060334k
A series of peptide analogs of Ac-CIYKYY (1) were synthesized by functional group modifications in peptide side chains or by introducing conformational constraints, to improve the inhibitory potency against active Src kinase. Ac-CIYKF(4-NO2)Y (2, IC50 = 0.53 M) and conformationally constrained peptide I (IC50 = 0.28 M) exhibited 750- and 1400-fold higher inhibitory activities, resp., vs. that of 1 (IC50 = 400 M). Compd. 2 exhibited a partial competitive inhibition pattern against ATP.
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~14 Citings
49. Reduction of carbonyl compounds with sodium borohydride in the presence of clays in aprotic solvents By Kumar, Anil; Chauhan, S. M. S. From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2006), 45B(4), 10381040. Language: English, Database: CAPLUS
The selective redn. of the carbonyl group of various arom. and aliph. compds. bearing different functional groups with Na borohydride in the presence of clay in aprotic solvents gives 72-93% corresponding alcs. ~0 Citings
50. Converting a weak peptide inhibitor of Src kinase to potent peptide inhibitors by systemic structural modification
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By Kumar, Anil; Wang, Yuehao; Sun, Gongqin; Parang, Keykavous From Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug. 28-Sept. 1, 2005 (2005), MEDI-405. Language: English, Database: CAPLUS
The design, synthesis, and evaluation of new compds. against Src tyrosine kinases are attractive due to the assocn. of Src tyrosine kinases activity with several diseases including cancer and osteoporosis. In contrast to ATP binding site, a few peptides have been identified as substrates for Src tyrosine kinases. Most of these peptide substrates are rather weak inhibitors with Km in high micromolar or in millimolar range. The best examples from these studies are peptides, Ac-YIYGSFK and Ac-CIYKYY, which were reported to be inhibitors of Src. Our radioactive kinase assay showed that Ac-YIYGSFK (IC50 = 570 M) and Ac-CIYKYY (IC50 = 400 M) were weak inhibitors of polyE4Y phosphorylation by active c-Src. We investigated whether by functional group modifications in the side chains of amino acids in Ac-CIYKYY, the inhibitory activity can be improved. The purpose of this study was to understand the structure-activity relationship of these compds. in order to develop novel Src inhibitors. Peptide Ac-CIYKF(NO2)Y, in which the nitrophenylalanine is located at position 5, exhibited a significantly higher inhibitory potency (IC50 = 0.53 M) by approx. 750-fold vs. Ac-CIYKYY. Addnl., compds. with substituted halogens exhibited significantly high inhibitory potencies in the order of I > Cl > F. For example, Ac-CIYKF(4-I)Y exhibited (IC50 = 0.78 M) approx. 510fold higher inhibitory potency than Ac-CIYKYY. Mol. modeling studies showed that the intramol. hydrogen bonding of the amino group of the K4 with hydroxyl group of Y5 in Ac-CIYKYY is eliminated when the hydroxyl group is substituted with nitro group or halogens. It appears that the free amino group of the lysine is required for the interaction with the kinase domain of Src and generating inhibition. These results suggest that it is possible to convert a weak peptide inhibitor of Sc kinase to potent peptide inhibitors by systemic structural modifications. ~0 Citings
51. N-Heteroaromatic-peptide conjugates as Src kinase inhibitors By Kumar, Anil; Wang, Yuehao; Sun, Gonquin; Parang, Keykavous From Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug. 28-Sept. 1, 2005 (2005), MEDI-404. Language: English, Database: CAPLUS
Src kinase exists as intriguing therapeutic target for drug discovery with respect to cancer and osteoporosis. Although selective inhibitors competitive with ATP have been synthesized for specific protein kinases, the process of inhibitor development is labor intensive due mainly to the presence of a large no. of protein kinases that show a conserved ATP binding site. The main objective of this study was to exploit the ATP-binding site mol. recognition motif in combination with other recognition motifs. 3-Phenylpyrazolopyrimidine deriv., substituted with an alkyl carboxylic acid at N1 endocyclic amine, exhibited weak inhibitory potency (IC50 = 250 M). Addnl., the radioactive kinase assay using polyE4Y as the substrate suggested that peptides YIYGSFK (IC50 = 570 M) and Ac-CIYKYY (IC50 = 400 M) were weak inhibitors of polyE4Y phosphorylation by active c-Src. More than fifty N-heteroarom.-peptide conjugates were synthesized using 3-pyrazolopyrimidine deriv. as an ATP mimic and CIYKYY and YIYGSFK as peptide substrates. The carboxylic acid of substituted 3-phenylpyrazolopyrimidines was attached to the side chain of different amino acids in the peptide template. Two N-terminal substituted 3-phenylpyrazolopyrimidine-peptide conjugates, 3phenylpyrazolopyrimidine-CIYKYY (IC50 = 0.38 M) and 3-phenylpyrazolopyrimidine-YIYGSFK (IC50 = 2.7 M), inhibited the polyE4Y phosphorylation by active Src significantly higher than parent compds., N-heteroaroms. and
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peptides. This study suggests a synergistic inhibition effect of the conjugation of the ATP mimic with the peptide by possibly creating favorable interactions between the conjugate and the kinase domain. Mol. modeling studies of 3phenylpyrazolopyrimidine-CIYKYY conjugate with Src suggested that the pyrazolopyrimidine ring binds to the ATP binding site and the peptide occupies the exterior space of the N-lobe in the kinase domain creating some new bonding interactions. This study suggests that weak inhibitors of Sc kinase can be conjugated to generate potent lead inhibitors that may be used for further optimization. ~0 Citings
52. Conformationally constrained peptide analogs of CIYKYY as inhibitors of Src tyrosine kinase By Ye, Guofeng; Kumar, Anil; Wang, Yuehao; Sun, Gongqin; Parang, Keykavous From Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug. 28-Sept. 1, 2005 (2005), MEDI-403. Language: English, Database: CAPLUS
Peptide Ac-CIYKYY was a weak inhibitor (IC50 = 400 M) of polyE4Y phosphorylation by active Src as shown by the radioactive kinase assay. Peptide Ac-CIYKF(NO2)Y, in which the nitrophenylalanine is located at Y5 position, exhibited a significantly higher inhibitory potency (IC50 = 0.53 M) by approx. 750-fold vs. Ac-CIYKYY. Conformationally constrained derivs. of these compds. were synthesized by solid-phase methods to det. whether the presence of the constrained ring has any effect in inhibitory potency. Due to the presence of three tyrosine residues and one lysine in the C1I2Y3K4Y5Y6, there were several opportunities for linking side chains of amino acids. Four types of conformational constraints were introduced by linking head to tail, C-terminal to side chain, N-terminal to side chain, and side chain to side chain of the amino acids. The structure-activity relationships of these analogs and the comparison of their inhibitory potency with parent linear peptides are discussed. ~0 Citings
53. Synthesis and evaluation of hydroxamate derivatives as metal-mediated inhibitors of Csk By Gu, Xianfeng; Wang, Yuehao; Kumar, Anil; Sun, Gonquin; Parang, Keykavous From Abstracts of Papers, 230th ACS National Meeting, Washington, DC, United States, Aug. 28-Sept. 1, 2005 (2005), MEDI-378. Language: English, Database: CAPLUS
In order to explore the possibility of designing metal-mediated inhibitors against protein tyrosine kinases, a class of tyrosine and phenylalanine hydroxamate derivs. were synthesized (25 compds.) and evaluated for their ability to inhibit C-terminal Src kinase (Csk), a model tyrosine kinase, in the presence of cobalt. Tyrosine hydroxamate (IC50 = 9.5 M) and phenylalanine hydroxamate (IC50 = 15.5 M) inhibited Csk only in the presence of CoCl2. The presence of bulky groups (e.g., Cl, Br, I) or pyrazolopyrimidine on the Ph ring enhanced the inhibitory potency (IC50 = 2.0-6.3 M), possibly due to the presence of interactions between these groups and a hydrophobic pocket in the enzyme. The substitution of amino group of hydroxamate with alkyl or aryl groups or removal of -amino group significantly reduced the inhibitory potency. These data suggest that specific functional groups are required for metal-binding
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affinity and inhibitors with better inhibitory profile can be designed. ~0 Citings
54. Microwave-assisted aromatic nucleophilic substitution reaction of chloronitrobenzenes with amines in ionic liquids By Angrish, Chetna; Kumar, Anil; Chauhan, S. M. S. From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2005), 44B(7), 15151518. Language: English, Database: CAPLUS
An efficient method for arom. nucleophilic substitution reaction of chloronitrobenzenes with several substituted amines in environmentally benign, 1-butyl-3-methylimidazolium tetrafluoroborate ionic liq. under microwave irradn. in reduced time period and high yields was described. ~4 Citings
55. Functional Diversity of Csk, Chk, and Src SH2 Domains due to a Single Residue Variation By Ayrapetov, Marina K.; Nam, Nguyen Hai; Ye, Guofeng; Kumar, Anil; Parang, Keykavous; Sun, Gongqin From Journal of Biological Chemistry (2005), 280(27), 25780-25787. Language: English, Database: CAPLUS, DOI:10.1074/jbc.M504022200
The C-terminal Src kinase (Csk) family of protein tyrosine kinases contains two members: Csk and Csk homologous kinase (Chk). Both phosphorylate and inactivate Src family kinases. Recent reports suggest that the Src homol. (SH) 2 domains of Csk and Chk may bind to different phosphoproteins, which provides a basis for different cellular functions for Csk and Chk. To verify and characterize such a functional divergence, we compared the binding properties of the Csk, Chk, and Src SH2 domains and investigated the structural basis for the functional divergence. First, the study demonstrated striking functional differences between the Csk and Chk SH2 domains and revealed functional similarities between the Chk and Src SH2 domains. Second, structural anal. and mutagenic studies revealed that the functional differences among the three SH2 domains were largely controlled by one residue, Glu127 in Csk, Ile167 in Chk, and Lys200 in Src. Mutating these residues in the Csk or Chk SH2 domain to the Src counterpart resulted in dramatic gain of function similar to Src SH2 domain, whereas mutating Lys200 in Src SH2 domain to Glu (the Csk counterpart) resulted in loss of Src SH2 function. Third, a single point mutation of E127K rendered Csk responsive to activation by a Src SH2 domain ligand. Finally, the optimal phosphopeptide sequence for the Chk SH2 domain was detd. These results provide a compelling explanation for the functional differences between two homologous protein tyrosine kinases and reveal a new structure-function relationship for the SH2 domains. ~4 Citings
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56. Synthesis of transition metal porphyrins from free-base 5,10,15,20-tetraarylporphyrins under microwave irradiation in ionic liquids By Jain, Nidhi; Kumar, Anil; Chauhan, S. M. S. From Synthetic Communications (2005), 35(9), 1223-1230. Language: English, Database: CAPLUS, DOI:10.1081/SCC-200054823
An efficient method for the synthesis of metalloporphyrins in 71-98% yields from free-base 5,10,15,20tetraarylporphyrins in ionic liqs. under microwave irradn. was described. 1-Butyl-3-methylimidazolium tetrafluoroborate, (bmim)(BF4), was chosen for use as the ionic liq. Ten metalloporphyrins were prepd., [(TPP)MCl] (M = Fe, Mn), [(TPP)M] (M = Co, Cu, Zn) and [(L)MnCl] (H2L = 5,10,15,20-tetraarylporphyrins with aryl = 4chlorophenyl, 4-nitrophenyl, 2,6-dichlorophenyl, 2,4,6-trimethylphenyl and pentafluorophenyl). ~10 Citings
57. Metalloporphyrin and heteropoly acid catalyzed oxidation of CNOH bonds in an ionic liquid: biomimetic models of nitric oxide synthase By Jain, Nidhi; Kumar, Anil; Chauhan, Shive M. S. From Tetrahedron Letters (2005), 46(15), 2599-2602. Language: English, Database: CAPLUS, DOI:10.1016/j.tetlet.2005.02.088
Water sol. iron(III) porphyrins and phosphotungstic acid in an ionic liq. are effective catalysts for the H2O2 mediated oxidn. of the C=NOH bond in N-hydroxyarginine and other oximes. The carbonyl compds. generated as the oxidn. products can be easily isolated from the reaction media. These systems serve as biomimetic models of nitric oxide synthase (NOS) and the catalyst immobilized in an ionic liq. can be easily recycled and reused. ~51 Citings
58. Chemical and biochemical transformations in ionic liquids By Jain, Nidhi; Kumar, Anil; Chauhan, Sushma; Chauhan, S. M. S. From Tetrahedron (2005), 61(5), 1015-1060. Language: English, Database: CAPLUS, DOI:10.1016/j.tet.2004.10.070
A review. Synthesis of ionic liqs., transition metal-catalyzed reactions in ionic liqs., org. reactions in ionic liqs., and biochem. transformations in ionic liqs. are included. Some of the reactions included are Friedel-Crafts reaction, DielsAlder reaction, Knoevenagel condensation reaction, Baylis-Hillman reaction, and fluorination. ~444 Citings
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59. 1-methyl-3-butylimidazolium decatungstate in ionic liquid. An efficient catalyst for the oxidation of alcohols By Chhikara, Bhupender S.; Tehlan, Sarita; Kumar, Anil From Synlett (2005), (1), 63-66. Language: English, Database: CAPLUS, DOI:10.1055/s-2004-836027
An excellent system for the selective oxidn. of benzylic and secondary alcs. with hydrogen peroxide catalyzed by 1methyl-3-butylimidazolium decatungstate in [bmim][BF4] ionic liq. is described. The catalytic system is reusable and products are obtained in excellent yield under environmentally benign conditions. ~29 Citings
60. Ytterbium(III) triflate-catalyzed conversion of carbonyl compounds into 1,3-oxathiolanes in ionic liquids By Kumar, Anil; Jain, Nidhi; Rana, Sandeep; Chauhan, Shive M. S. From Synlett (2004), (15), 2785-2787. Language: English, Database: CAPLUS, DOI:10.1055/s-2004-835642
The reaction of carbonyl compds. with 2-mercaptoethanol to prep. 1,3-oxathiolanes was successfully carried out in ionic liqs. using ytterbium(III) triflate as a catalyst. Yields of the products are high and the catalyst can be easily recovered and reused in this reaction. ~24 Citings
61. Oxidation of benzylic alcohols to carbonyl compounds with potassium permanganate in ionic liquids By Kumar, Anil; Jain, Nidhi; Chauhan, S. From Synthetic Communications (2004), 34(15), 2835-2842. Language: English, Database: CAPLUS, DOI:10.1081/SCC-200026242
The selective oxidn. of primary and secondary benzylic alcs. with potassium permanganate in ionic liqs. to give corresponding aldehydes and ketones in 83-97% yields was described. ~14 Citings
62. -Polynitration of 5,10,15,20-tetrakis(2',6'-Dichlorophenyl)porphyrins with HNO3 and Cu(NO3)2 on Clay Using Microwave Irradiation By Chauhan, S.; Kumar, Anil; Srinivas, K. A.
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From Synthetic Communications (2004), 34(14), 2673-2680. Language: English, Database: CAPLUS, DOI:10.1081/SCC-200025635
An expeditious -polynitration of 5,10,15,20-tetrakis(2',6'-dichlorophenyl)porphyrin and its Zn and Cu derivs. with montmorillonite K10-HNO3 and montmorillonite K10-Cu(NO3)2 (claycop) under mild conditions using microwave irradn. in 72-95% yields has been described. ~4 Citings
63. Effect of side chain length on the aggregation of amphiphilic 5,10,15-tris (1-methylpyridinium-4-yl)-20-[4alkoxyphenyl]-21H,23H porphyrin tritosylates By Chauhan, S. M. S.; Kumar, Anil; Srinivas, K. A.; Mishra, M. K. From Indian Journal of Biochemistry & Biophysics (2003), 40(6), 429-438. Language: English, Database: CAPLUS
Self-aggregation of cationic amphiphilic 5,10,15-tris-(1-methylpyridinium-4-yl)-20-[4-alkoxyphenyl]-21H,23H-porphyrin tritosylates I (X- = 4-MeC6H4SO3-, R = (CH2)nMe, n = 0, 5, 9, 15, 17) with different alkoxy chain length in aq. and binary solvent systems has been studied by UV-visible, fluorescence and 1H NMR spectroscopy. Binary solvent, concn., ionic strength, presence of surfactants, and temp. govern the aggregations of I (X- = 4-MeC6H4SO3-, R = (CH2)nMe, n = 0, 5, 9, 15, 17). Porphyrins having side chain length more than ten carbon atoms I (X- = 4MeC6H4SO3-, R = (CH2)nMe, n = 9, 15, 17) form higher aggregates, such as vesicles by sonication of dimers formed initially, whereas porphyrins with lesser side chain length I (X- = 4-MeC6H4SO3-, R = (CH2)nMe, n = 0, 5) form lower aggregates only. Further, the size and the formation of vesicles have been confirmed by transmission electron microscopy (TEM) and dye entrapment expts. for I (X- = 4-MeC6H4SO3-, R = (CH2)nMe, n = 17).
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~3 Citings
64. Isolation and characterization of selected secondary metabolites from dry leaves of Quercus semicarpifolia By Chauhan, S. M. S.; Singh, Mamta; Kumar, Anil From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2004), 43B(1), 223226. Language: English, Database: CAPLUS
Nonacosane, friedelin, -sitosterol, and oleanolic acid have been isolated from petroleum ether ext. of Quercus semicarpifolia dry leaves, as well as 5-acetoxy-3,3',4',5'-tetramethoxyflavone - from acetone ext. and quercetin - from methanolic ext. ~3 Citings
65. Synthesis and characterization of nano/ultrafine sized silver bromide particles in microemulsions
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By Kumar, Anil; Sharma, Parvesh; Saxena, Amit; Patanjali, P. K. From Journal of Surface Science and Technology (2003), 19(1-2), 35-48. Language: English, Database: CAPLUS
Ag bromide nanoparticles of different sizes down to 5nm in diam. were synthesized by mixing 2 microemulsions contg. the precursor salts AgNO3 and KBr. The microemulsions used in the synthesis are composed of Triton X-100/1hexanol/cyclohexane/H2O. This study focused on the various parameters controlling the size of Ag bromide particles in nanometer range, such as W0 and concn. of the precursor salts. The size and morphol. of the particles were ascertained by QELS and TEM. The size of nanoparticles was always larger than the size of the aq. core in which they are formed. In the W0 range, 5-20, there is an increase in the particle size with increase of the H2O pool size. However, with the increase in the concn. of either Ag+ ion or Br- ion, the size of the AgBr nanoparticles decreased significantly. Also the morphol. of the particles was not always the same and depends upon the reaction conditions at which the synthesis is carried out. ~1 Citing
66. Biomimetic oxidation of curcumin with hydrogen peroxide catalyzed by 5,10,15,20-tetraarylporphyrinatoiron(III) chlorides in dichloromethane By Chauhan, Shive Murat Singh; Kandadai, Appan Srinivas; Jain, Nidhi; Kumar, Anil From Chemical & Pharmaceutical Bulletin (2003), 51(11), 1345-1347. Language: English, Database: CAPLUS, DOI:10.1248/cpb.51.1345
The biomimetic oxidn. of curcumin, a main turmeric pigment with hydrogen peroxide catalyzed by different 5,10,15,20tetraarylporphyrinatoiron(III) chlorides [TAPFe(III)Cl] in dichloromethane has been studied to give a C-C coupled curcumin dimer (I) in 40-70% yield. The structure of I has been elucidated by 1H-, 13C-NMR, IR and FAB-Mass spectroscopic data.
~9 Citings
67. Deprotection of 1,3-oxathiolanes to carbonyl compounds with montmorillonite K10 By Chauhan, S. M. S.; Kumar, Anil; Sahoo, B. B. From Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (2003), 42B(10), 2635-2637. Language: English, Database: CAPLUS
Montmorillonite K10 was used in the deprotection of different arom. and aliph. 1,3-oxathiolanes to the corresponding carbonyl compds. in 73 to 97% yields under mild and environmentally compatible conditions. ~3 Citings
68. Copper(I) chloride catalyzed synthesis of diaryl ethers in ionic liquids under mild conditions By Chauhan, S. M. S.; Jain, Nidhi; Kumar, Anil; Srinivas, K. A. From Synthetic Communications (2003), 33(20), 3607-3614. Language: English, Database: CAPLUS, DOI:10.1081/SCC-120024748
The reaction of different aryl halides with aryl oxides catalyzed by CuCl in 1-butyl-3-methylimidazolium tetrafluoroborate [bmim][BF4] and 1-butyl-3-methylimidazolium hexafluorophosphate [bmim][PF6] ionic liqs. to give diaryl ethers in 54-90% yields was studied under mild reaction conditions. ~19 Citings
69. Oxidation of thiols with molecular oxygen catalyzed by cobalt(II) phthalocyanines in ionic liquid By Chauhan, S. M. S.; Kumar, Anil; Srinivas, K. A. From Chemical Communications (Cambridge, United Kingdom) (2003), (18), 2348-2349. Language: English, Database: CAPLUS, DOI:10.1039/b305888c
An efficient procedure for catalyst soly., recycling and easy product isolation in oxidn. of thiols to disulfides with mol. oxygen catalyzed by cobalt(II) phthalocyanines dissolved in ionic liq. at room temp. is reported. The catalysts, [2,9,16,23-tetranitro-29H,31H-phthalocyaninato(2-)-N29,N30,N31,N32]cobalt and [29H,31H-phthalocyaninato(2-)N29,N30,N31,N32]cobalt, are immobilized in the ionic liq. 1-butyl-3-methyl-1H-imidazolium tetrafluoroborate(1-) and are easily recyclable. ~61 Citings
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70. Phase behavior and characterization of various microdomains in pseudo-ternary Triton X-100 + 1hexanol/aqueous electrolyte/oil systems By Kumar, Anil; Saxena, Amit; Mozumdar, S.; Patanjali, P. K. From Journal of Surface Science and Technology (2002), 18(3-4), 139-152. Language: English, Database: CAPLUS
Several microemulsion microstructures were identified in the aq. phase region of Triton X-100/1-hexanol/aq. electrolyte/oil systems by cond., viscosity, and quasi-elastic light scattering measurements. Effects of various parameters such as bulk oil, electrolyte concn. and temp. on the microstructures of the above systems were studied. The phase diagram with cyclohexane is a combination of large one phase isotropic region and a small mesophase of liq. cryst. gel. In the dodecane system, the addn. of NaCl has made the mesophase disappear with an extension of the one phase region towards the H2O axis. The single phase isotropic region consisted of oil-in-H2O microemulsion and H2O-in-oil microemulsion sepd. by a bicontinuous microemulsion. In the upper high surfactant-co-surfactant concn. region, the system seemed to be consisting of small hydrated reverse aggregate of Triton X-100 dispersed in hexanol and oil medium. Optimum salinity of the above systems had a major dependence on the amt. of electrolyte added and a minor dependence on temp. ~0 Citings
71. High frequency noise in fully overlapped lightly doped drain MOSFETs By Kumar, Anil; Haldar, Subhasis; Gupta, Mridula; Gupta, R. S. From Microelectronic Engineering (2003), 65(3), 249-257. Language: English, Database: CAPLUS, DOI:10.1016/S0167-9317(02)00886-9
The high frequency noise of fully overlapped lightly doped drain (FOLD) MOSFETs incorporating the field dependent mobility and the bias dependent series resistance is predicted. This includes the thermal noise and the induced gate noise. The results so obtained for effective current noise gain are compared with the simulated data of short channel LDD MOSFETs and are in good agreement. At frequencies much below the cut-off frequency, the induced gate noise is just 1% or even less of the drain noise. The effective current noise gain in FOLD and LDD MOSFETs is compared and shows that thermal noise increases while gate induced noise decreases with the decrease in channel length. ~1 Citing
72. Development and characterization of a novel immobilized microbial membrane for rapid determination of biochemical oxygen demand load in industrial waste-waters By Rastogi, Shikha; Kumar, Anil; Mehra, N. K.; Makhijani, S. D.; Manoharan, A.; Gangal, V.; Kumar, Rita From Biosensors & Bioelectronics (2003), 18(1), 23-29. Language: English, Database: CAPLUS, DOI:10.1016/S09565663(02)00108-2
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The rapid detn. of wastewater quality of wastewater treatment plants in terms of pollutional strength, i.e. BOD is difficult or even impossible using the chem. detn. method. The study reports the detn. of BOD within minutes using microbial BOD sensors, as compared to the 5-day detn. using the conventional method. Multiple criteria establish the basis for the development of a BOD biosensor useful for rapid and reliable BOD estn. in industrial wastewaters. Of these, prepn. of a suitable novel immobilized microbial membrane used in conjunction with an apt transducer is discussed. As a result, a microbial biosensor based on a formulated, synergistic, pre-tested microbial consortium was developed for the measurement of BOD load of various industrial wastewaters. The sensor showed max. response in terms of current difference, when a cell concn. of 2.25 1010 CFU, harvested in their log phase of growth were utilized for microbial membrane construction. The sensor showed a stability of 180 days when the prepd. membranes were stored at a temp. of 4 in 50 mM phosphate buffer of pH 6.8. The reusability of the immobilized membranes was 200 cycles without appreciable loss of their response characteristics. A linear relationship between the current change and a glucose-glutamic acid (GGA) concn. 60 mg L-1 was obsd. (r = 0.999). The lower detection limit was 1.0 mg L-1 BOD. The sensor response was reproducible within 5% of the mean in a series of 10 samples having 44 mg L-1 BOD using std. a GGA soln. When used for the BOD estn. of industrial wastewaters, a relatively good agreement was found between the 2 methods, i.e. 5-day BOD and that measured by the developed microbial sensor. ~36 Citings
73. Biomimetic reduction of nimesulide with NaBH4 catalyzed by metalloporphyrins By Chauhan, Shive Murat Singh; Kandadai, Srinivas Appan; Kumar, Anil From Chemical & Pharmaceutical Bulletin (2002), 50(10), 1421-1422. Language: English, Database: CAPLUS, DOI:10.1248/cpb.50.1421
The biomimetic redn. of the anti-inflammatory drug, nimesulide with sodium borohydride catalyzed by 5,10,15,20tetraarylporphyrinatoiron(III) chlorides [TAPFe(III)Cl] has been studied in org. solvents under anaerobic and aerobic conditions. ~3 Citings
74. Epoxidation of alkenes with hydrogen peroxide catalyzed by iron(III) porphyrins in ionic liquids By Srinivas, K. A.; Kumar, Anil; Chauhan, S. M. S. From Chemical Communications (Cambridge, United Kingdom) (2002), (20), 2456-2457. Language: English, Database: CAPLUS, DOI:10.1039/b207072n
An efficient procedure is described for catalyst recycling and easy product isolation in alkene epoxidn. with hydrogen peroxide catalyzed by water-sol. iron(III) porphyrins in environmentally benign and ambient temp. ionic liqs.
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~64 Citings
75. Analytical model for saturation drain current and substrate current of fully overlapped LDD MOSFET By Kumar, Anil; Kalra, Ekta; Bose, Srikanta; Singh, Adarsh; Bindra, Simrata; Haldar, Subhasis; Gupta, R. S. From Indian Journal of Pure and Applied Physics (2001), 39(11), 731-737. Language: English, Database: CAPLUS
An anal. model for satn. drain current and substrate current of fully overlapped lightly doped drain (LDD) MOSFET is developed using pseudo-two-dimensional approxn. in the channel and drain regions and expression of max. elec. field is obtained. An expression for channel length modulation factor is also developed and the substrate current is calcd. ~0 Citings
76. Characterization of small geometry LDD MOSFETs with non-pinned flatband voltage By Kalra, Ekta; Kumar, Anil; Haldar, Subhasis; Gupta, R. S. From Indian Journal of Pure and Applied Physics (2000), 38(8), 552-557. Language: English, Database: CAPLUS
A semi-empirical model to analyze the small geometry (short and narrow) effects in lightly doped drain (LDD) MOSFETs incorporating the dependence of flatband voltage on channel length and width is developed. The anal. includes the short channel, narrow width, LDD and DIBL effects. An expression for threshold voltage based on the effective charge contained in the channel is obtained and the results so obtained are in good agreement with the exptl. data. 1/F noise is also evaluated incorporating the voltage drop in n- region and charge induced due to flatband voltage, which matches well with exptl. data. ~0 Citings
77. 1/f Noise model of fully overlapped lightly doped drain MOSFET By Kumar, Anil; Kalra, Ekta; Haldar, Subhasis; Gupta, R. S. From IEEE Transactions on Electron Devices (2000), 47(7), 1426-1430. Language: English, Database: CAPLUS, DOI:10.1109/16.848287
This paper presents an anal. 1/f noise model of fully overlapped lightly doped drain MOSFET incorporating the voltage drop in the n- region due to the parasitic resistance. The fully overlapped lightly doped drain structure has lesser noise effect than lightly doped drain MOSFET and the predicted results are verified with exptl. data. ~4 Citings
78. An analytical model for electrical characteristics of short geometry LDD and short channel FOLD MOSFETs By Kumar, Anil; Kalra, Ekta; Haldar, Subhasis; Gupta, R. S. From Proceedings - International Conference on Microelectronics, 22nd, Nis, Yugoslavia, May 14-17, 2000 (1999), 1, 213-216. Language: English, Database: CAPLUS
An anal. model for elec. characteristics of short geometry lightly doped drain (LDD) MOSFET and short channel fully overlapped LDD (FOLD) MOSFET is developed. The results obtained using this model are in good agreement with the exptl. data showing the validity of the model in the submicrometer range. ~0 Citings
79. Suppression of residual hydrophobicity of amphiphilic amino acids by forming association complexes with cyclodextrin By Kumar, Anil; Maitra, Amarnath From Journal of the Indian Chemical Society (1996), 73(10), 516-519. Language: English, Database: CAPLUS
The interfacial tension at the benzene/water interface has been studied in the presence of four amphiphilic amino acids, viz. alanine, phenylalanine, valine and leucine in presence and in absence of -cyclodextrin. The interfacial tension which is otherwise decreased with the increased concn. of amino acids, was found to increase gradually with progressive addn. of cyclodextrin. The results have been explained on the basis of inclusion complexation between the hydrocarbon side-chain of the amino acid and cyclodextrin. The formation consts. and other thermodn. parameters have been evaluated for the inclusion complexes. It has been concluded that long and straight hydrocarbon side-chains are preferably included into the cavity of cyclodextrin mol. ~2 Citings
80. Effect of laser-irradiation on structural and electrical properties of cadmium sulfide thin films By Dawar, A. L.; Shishodia, P. K.; Chauhan, Gayatri; Kumar, Anil; Mathur, P. C. From Journal of Applied Physics (1990), 67(10), 6214-19. Language: English, Database: CAPLUS, DOI:10.1063/1.345187
CdS films were deposited by a resistive heating technique onto glass substrates kept at 150. The films were irradiated with laser pulses of various energy densities. A pulsed laser (Nd-doped yttrium aluminum garnet) capable of producing a 20-ns pulse of 0.53 m wavelength (frequency doubled) with varying energy densities (2-50 mJ/cm2)
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was employed. X-ray diffraction studies showed that the crystallinity of the films improved with laser irradn., d.c. cond. and Hall coeff. measurements were made on the films at 77-300 K for both as-grown and laser-irradiated films. Both the Hall coeff. and mobility increased with an increase of energy d. as well as the no. of pulses. Typically, the mobility increased from 71 to 121 cm2V-1s-1 after irradn. with 50 laser pulses of energy d. 28 mJ/cm2. ~1 Citing
81. Effect of laser annealing on the structural, electrical and optical properties of cadmium telluride thin films By Dawar, A. L.; Jagadish, C.; Ferdinand, K. V.; Kumar, Anil; Mathur, P. C. From Applications of Surface Science (1977-1985) (1985), 22-23(2), 846-58. Language: English, Database: CAPLUS, DOI:10.1016/0378-5963(85)90218-1
CdTe films of 0.7 m thickness were deposited by using a resistive technique onto glass and KBr substrates kept at 200. The films were irradiated with laser pulses of various energy densities. A pulsed laser (Nd:YAG) capable of producing 20 ns pulses of wavelength 1.06 m with varying energy densities (2-50 mJ/cm2) was employed. The films were examd. by using TEM and x-ray diffraction and found polycryst. D.c. cond. and Hall coeff. were measured at 77400 K. The optical energy gap ws calcd. by using the optical transmission spectra. ~1 Citing
82. Field effect studies on MIS structures of n-type lead tin telluride (Pb0.8Sn0.2Te) thin films By Dawar, A. L.; Ferdinand, K. V.; Jagadish, C.; Kumar, Anil; Kumar, Partap; Mathur, P. C. From Applications of Surface Science (1977-1985) (1985), 22-23(2), 781-91. Language: English, Database: CAPLUS, DOI:10.1016/0378-5963(85)90211-9
D.c. cond. and Hall coeff. RH studies were made on MIS structures of n-type Pb0.8Sn0.2Te thin films grown by a flash evapn. technique in the temp. range 77-400 K. The decrease in RH with pos. gate field and increase in RH with neg. gate field are attributed to the accumulation and depletion of current carriers due to bending of bands. Mobility-temp. data are analyzed in terms of various scattering mechanisms. ~0 Citings
83. Field effect studies on MIS structures and effect of laser annealing on the structural, electrical and optical properties of lead tin telluride (Pb0.8Sn0.2Te) thin films By Dawar, A. L.; Jagadish, C.; Ferdinand, K. V.; Pal, Suranjan; Kumar, P.; Kumar, Anil; Mathur, P. C. From Surface Science (1985), 152-153(2), 1273-85. Language: English, Database: CAPLUS, DOI:10.1016/0039-
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6028(85)90548-5
Field effect studies on metal-insulator-semiconductor structures of Ag-mica-p-Pb0.8Sn0.2Te were made 77-400 K. The effect of neg. gate field is to decrease the Hall coeff. and Hall mobility, where the effect of pos. gate field is opposite. Results are explained on the basis of accumulation and depletion of current carriers. Films were annealed with 10-50 laser pulses of energy densities 4-30 mJ/cm2. TEM and x-ray diffraction studies were the structural changes which occurred due to laser annealing. Hall coeff. and Hall mobility studies were made on all the films and an increase in mobility was obsd. with laser annealing. Optical transmission studies were made on the films grown on KBr pellets. ~0 Citings
84. Field effect studies on MIS structures of p-type mercury cadmium telluride (Hg0.8Cd0.2Te) thin films By Dawar, A. L.; Ferdinand, K. V.; Jagadish, C.; Kumar, Anil; Mathur, P. C. From Extended Abstracts of the Conference on Solid State Devices and Materials (1984), 16th, 407-11. Language: English, Database: CAPLUS
Cond. (d.c.) and Hall-coeff. studies were made on MIS structures of Hg0.8Cd0.2Te thin films as functions of gate field and temp. (77-400 K). Decrease and increase in Hall coeff. and Hall mobility with heg. and pos. gate fields are attributed to the accumulation and depletion of majority carriers. The mobility-temp. data are analyzed in terms of different scattering mechanisms. ~0 Citings
85. Field-effect studies on p-type copper indium telluride (CuInTe2) metal-insulator-semiconductor structures By Dawar, A. L.; Kumar, Anil; Kumar, Partap; Mathur, P. C. From Journal of Applied Physics (1984), 55(10), 3695-8. Language: English, Database: CAPLUS, DOI:10.1063/1.332920
Field-effect studies on MIS structures of p-CuInTe2 thin films grown on mica were made at 77-295 K. An increase in carrier d. and a decrease in the mobility are obsd. on the application of a neg. gate field. The effect of a pos. gate field is the opposite. The Hall coeff. remains practically const. at a lower temp. range (77-180 K) and then decreases with further rise in temp. According to a study of the effective field-effect mobility FE, a surface states charge scattering mechanism dominates the scattering process. ~3 Citings
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86. Growth and electrical transport properties of copper indium telluride (CuInTe2) thin films By Dawar, A. L.; Kumar, Anil; Mall, R. P.; Mathur, P. C. From Thin Solid Films (1984), 112(2), 107-19. Language: English, Database: CAPLUS, DOI:10.1016/00406090(84)90488-7
The growth and elec.-transport properties at 77-295 K of thin films of CuInTe2 grown on mica and glass substrates and annealed in an Ar atm. were studied. As-grown films had high resistivity, and annealing of the films in Ar increased their cond. The annealed films were single-phase and polycryst. Films evapd. at rates from 60 to 80 s-1 had better elec. properties than films grown at higher evapn. rates. The d.c. cond. and Hall-coeff. data were analyzed to establish the conduction mechanism. ~5 Citings
87. Growth and electrical properties of cuprous telluride thin films By Dawar, A. L.; Kumar, Anil; Kumar, Partap; Mathur, P. C. From Journal of the Less-Common Metals (1983), 91(1), 83-8. Language: English, Database: CAPLUS, DOI:10.1016/0022-5088(83)90097-8
Polycryst. Cu2Te films were grown on mica substrates by vacuum evapn. at 350 and were then annealed at the same temp. in a vacuum for 2 h. The films, which were grown by using a stoichiometric charge, have large nos. of Cu vacancies. Hall coeff. and Hall mobility of these films were studied at 77-300 K. The variation in the Hall mobility with temp. indicated that the mobility is mainly limited by defect scattering and ionized impurity scattering at 77-200 K, while lattice scattering is predominant at >200 K. ~2 Citings
88. Effect of hydrogen on electrical transport properties of polycrystalline copper indium ditelluride thin films By Dawar, A. L.; Kumar, Anil; Kumar, Partap; Mathur, P. C. From Journal of Materials Science (1983), 18(3), 815-20. Language: English, Database: CAPLUS, DOI:10.1007/BF00745580
The effect of mol. H on the elec. transport properties of p-type CuInTe2 films was studied by exposing the films to high pressure (up to 700 psi). The Hall coeff. increased initially with increasing pressure up to 500 psi and then decreased. The mobility increased with gas pressure. The results are explained in terms of a grain-boundary scattering mechanism and in terms of donor action provided by H diffusion into the thin film. ~0 Citings
89. Field effect studies in indium telluride (In2Te3) metal-insulator-semiconductor structure By Dawar, A. L.; Kumar, Anil; Taneja, O. P.; Kumar, Partap; Mathur, P. C. From Physica Status Solidi A: Applied Research (1982), 74(2), 403-9. Language: English, Database: CAPLUS, DOI:10.1002/pssa.2210740204
Field-effect studies on MIS structures of Ag-sapphire-In2Te3 films were made at 77-295 K. An increase in carrier d. and a decrease in the mobility were obsd. on application of a pos. gate field. The effect of a neg. gate field is opposite. The results are explained in terms of accumulation and depletion of current carriers at the insulatorsemiconductor interface. ~1 Citing
90. Growth and properties of well-oriented indium telluride thin films By Mathur, P. C.; Kumar, Anil; Kumar, Partap From Thin Solid Films (1982), 88(3), 263-8. Language: English, Database: CAPLUS, DOI:10.1016/00406090(82)90055-4
Well-oriented thin films of In2Te3 were grown on sapphire substrates by thermal evapn. at 350 and were then annealed in an Ar atm. at 400 for 2 h. The d.c. cond. and Hall effect of these films were detd at 77-295 K. The variation in the Hall mobility with temp. indicated that there is a considerable contribution from lattice scattering above 220 K. ~10 Citings
91. Growth and electrical transport properties of indium telluride (In2Te3) thin films By Mathur, P. C.; Kumar, Anil; Taneja, O. P.; Dawar, A. L. From Thin Solid Films (1981), 78(4), 377-83. Language: English, Database: CAPLUS, DOI:10.1016/00406090(81)90041-9
Hall coeff. and d.c. cond. studies at 100-625 K were made on polycryst. In2Te3 films grown on glass and mica substrates. When the films were cycled above 525 K the cond. was irreversible; this is explained in terms of structural changes at high temp. The Hall mobilities of the films are independent of temp., showing the predominance of neutral impurity scattering over grain boundary scattering.
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~9 Citings
92. Temperature dependence of pressure broadened linewidths in the microwave region By Srivastava, G. P.; Kumar, Devendra; Kumar, Anil From Journal of Chemical Physics (1977), 66(1), 20-3. Language: English, Database: CAPLUS, DOI:10.1063/1.433666
Self-broadened linewidths of OCS, BrCN, MeBr, and HCHO were measured from -40 to 75 by using a double modulation microwave spectrograph. The linewidths were also calcd. by using Anderson-Tsao-Curnutte theory and the extension by J.. S. Murphy and J. E. Boggs (1967). Within the temp. range investigated the linewidth decreases with temp. both exptl. and theor. in an identical manner. ~2 Citings
93. Foreign gas broadening by the water molecule By Srivastava, G. P.; Kumar, Anil From Journal of Chemical Physics (1976), 65(1), 293-5. Language: English, Database: CAPLUS, DOI:10.1063/1.432767
Microwave spectral linewidths of OCS, BrCN, MeCN, HCHO, and C2H4O were measured as broadened by the water mol. on a double modulation microwave spectrograph. On comparing the exptl. linewidths with theor. calcd. linewidths on the basis of the P. W. Anderson (1949) as well as the J. S. Murphy-J. E. Boggs (1967) theory, it was found that the exptl. linewidths are higher than the calcd. ones, although the strong dipole interactions are involved. ~0 Citings
94. Microwave pressure broadening studies of ethylene oxide By Srivastava, G. P.; Kumar, Anil From Journal of Physics B: Atomic and Molecular Physics (1974), 7(18), 2578-90. Language: English, Database: CAPLUS, DOI:10.1088/0022-3700/7/18/022
Self broadening and foreign gas broadening of 8 transitions of ethylene oxide were studied exptl. as well as theor. The line width measurements were made on double modulation microwave spectrograph at room temp. Line widths were calcd. by using the theories of P. W. Anderson (1949) and J. S. Murphy and J. E. Boggs (1967). Theor. and exptl. results were compared. The variation of line width with the quantum no. of transitions also was studied. An
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attempt was made to correlate the exptl. and theor. results. ~0 Citings
95. Pressure broadened line widths of cyanogen bromide in the microwave region By Srivastava, G. P.; Kumar, Anil; Kumar, Devendra From Molecular Physics (1973), 26(3), 693-8. Language: English, Database: CAPLUS, DOI:10.1080/00268977300102001
The line widths of BrCN were measured at 305K by using a double modulation microwave spectrograph. The selfbroadening of 2 quadrupole hyperfine lines of the transition J = 3 4 were measured. The foreign gas broadening by COS, CO2, N2, MeCN, MeI, HCHO, and MeCHO were measured only for the intense line at 32.957 GHz. These measured line widths were compared with the calcd. linewidths by using the pressure-broadening theories of Anderson as well as of Murphy and Boggs. ~1 Citing
96. Microwave pressure broadening studies of some molecules By Srivastava, G. P.; Gautam, H. O.; Kumar, Anil From Journal of Physics B: Atomic and Molecular Physics (1973), 6(4), 743-56. Language: English, Database: CAPLUS, DOI:10.1088/0022-3700/6/4/027
The line width of COS, MeCN, and HCHO were measured at room temp. by using a double modulation microwave spectrometer. Twenty cases of self-broadening and foreign gas broadening were studied. The exptl. results were compared with the calcd. results by using the impact theory of Anderson and collision broadening theory of Murphy and Boggs. The exptl. results were in good agreement with the theor. values of line width parameter for linear mols. In case of symmetric mols., the theor. results were higher than the exptl. obsd. results. The quadrupole moments of COS, CO2 and N2 were obtained from these measurements. The obsd. results agree better with Murphy and Boggs theory than with Anderson's theory. ~4 Citings
97. Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities By Rao Vagicherla Kameshwara; Rao Madharam Sudershan; Jain Navin; Panwar Jitendra; Kumar Anil From Organic and medicinal chemistry letters (2011), 1(1), 10, Language: English, Database: MEDLINE ABSTRACT: An efficient, one-pot synthesis was developed for 3-aminoalkylated indoles by three-component coupling
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reaction of aldehydes, N-methylanilines, and indoles using AgOTf as a catalyst. A series of twenty 3-aminoalkylated indoles was evaluated for their antibacterial activities against both Gram negative and Gram positive bacteria. Compounds 4b and 4r showed good antibacterial activity against both Gram positive and Gram negative strains. However, inversing the property of substituent (from 4r to 4q) resulted in the significant fall in the magnitude of antibacterial activity against Escherichia coli. ~0 Citings
Copyright 2012 U.S. National Library of Medicine.
98. Ionic liquid-supported synthesis of sulfonamides and carboxamides By Muthayala Manoj Kumar; Chhikara Bhupender S; Parang Keykavous; Kumar Anil From ACS combinatorial science (2012), 14(1), 60-5, Language: English, Database: MEDLINE An ionic liquid-supported aldehyde was designed and converted to ionic liquid-supported secondary aryl amines through reductive amination. The reaction of ionic liquid-supported aryl amines with sulfonyl chlorides and acid chlorides, respectively, followed by cleavage using trifluoroacetic acid (TFA) afforded sulfonamides and caboxamides. To introduce additional diversity in the synthesis of sulfonamides and caboxamides, ionic liquid-supported iodosubstituted aryl amine was synthesized using the same strategy, and underwent Suzuki coupling reaction, followed by reaction with a methanesulfonyl chloride to generate the corresponding biaryl sulfonamide. The advantages of the protocol over solid-phase synthesis are homogeneous reaction medium, high loading, easy separation of products, and characterization of intermediates. ~0 Citings
99. One-pot regioselective synthesis of tetrahydroindazolones and evaluation of their antiproliferative and Src kinase inhibitory activities By Rao V Kameshwara; Chhikara Bhupender S; Tiwari Rakesh; Shirazi Amir Nasrolahi; Parang Keykavous; Kumar Anil From Bioorganic & medicinal chemistry letters (2012), 22(1), 410-4, Language: English, Database: MEDLINE A number of 2-substituted tetrahydroindazolones were synthesized by three-component condensation reaction of 1,3diketones, substituted hydrazines, benzaldehydes, and Yb(OTf)(3) as a catalyst in [bmim][BF(4)] ionic liquid using a simple, efficient, and economical one-pot method. The synthesized tetrahydroindazolones were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and cSrc kinase activity. 3,4-Dichlorophenyl tetrahydroindazolone derivative (15) inhibited the cell proliferation of HT-29 and SK-OV-3 cells by 62% and 58%, respectively. 2,3-Diphenylsubstituted tetrahydroindazolone derivatives, inhibited the cell proliferation of HT-29 cells by 65-72% at a concentration of 50 M. In general, the tetrahydroindazolones showed modest inhibition of c-Src kinase where 4-tertbutylphenyl- and 3,4-dichlorophenyl- derivatives showed the inhibition of c-Src kinase with IC(50) values of 35.1 and 50.7 M, respectively. ~0 Citings
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100. 3-substitued indoles: one-pot synthesis and evaluation of anticancer and Src kinase inhibitory activities By Rao V Kameshwara; Chhikara Bhupender S; Shirazi Amir Nasrolahi; Tiwari Rakesh; Parang Keykavous; Kumar Anil From Bioorganic & medicinal chemistry letters (2011), 21(12), 3511-4, Language: English, Database: MEDLINE An efficient and economical method was developed for the synthesis of 3-substituted indoles by one-pot threecomponent coupling reaction of a substituted or unsubstituted benzaldehyde, N-methylaniline, and indole or Nmethylindole using Yb(OTf)(3)-SiO(2) as a catalyst. All the synthesized compounds were evaluated for inhibition of cell proliferation of human colon carcinoma (HT-29), human ovarian adenocarcinoma (SK-OV-3), and c-Src kinase activity. The 4-methylphenyl (4o and 4p) and 4-methoxyphenyl (4q) indole derivatives inhibited the cell proliferation of SK-OV-3 and HT-29 cells by 70-77% at a concentration of 50 M. The unsubstituted phenyl (4d) and 3-nitrophenyl (4l) derivatives showed the inhibition of c-Src kinase with IC(50) values of 50.6 and 58.3 M, respectively. ~0 Citings
101. Fatty acyl amide derivatives of doxorubicin: synthesis and in vitro anticancer activities By Chhikara Bhupender S; St Jean Nicole; Mandal Deendayal; Kumar Anil; Parang Keykavous From European journal of medicinal chemistry (2011), 46(6), 2037-42, Language: English, Database: MEDLINE Doxorubicin is extensively used in anticancer therapy. Doxorubicin is highly hydrophilic, has short half-life, and its use is associated with severe side effects at high doses. Fatty acyl amide derivatives of doxorubicin were synthesized with the expectation to improve the lipophilicity and anticancer activity of the drug. The lipophilicity was enhanced with the increase in chain length of fatty acyl moiety. Conjugation of 4'-amino group with fatty acids through an amide bond reduced the anticancer activity in leukemia, breast, ovarian, and colon cancer cell lines, suggesting that the presence of free amino group is required for anticancer activity of doxorubicin. Dodecanoyl-doxorubicin derivative was consistently the most effective among the synthesized derivatives and inhibited the proliferation of colon (HT-29) and ovarian (SK-OV-3) cancer cells by 64% and 58%, respectively, at a concentration of 1 M after 96 h incubation. ~0 Citings
102. Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities By Kumar Anil; Ahmad Israr; Chhikara Bhupender S; Tiwari Rakesh; Mandal Deendayal; Parang Keykavous From Bioorganic & medicinal chemistry letters (2011), 21(5), 1342-6, Language: English, Database: MEDLINE A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC(50) value of 5.6 M. 4-Methoxyphenyl triazolylsubstituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 M.
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103. Synthesis, antiviral and contraceptive activities of nucleoside-sodium cellulose sulfate acetate and succinate conjugates By Agarwal Hitesh K; Kumar Anil; Doncel Gustavo F; Parang Keykavous From Bioorganic & medicinal chemistry letters (2010), 20(23), 6993-7, Language: English, Database: MEDLINE Chemical conjugates between sodium cellulose sulfate (CS), displaying contraceptive and HIV-entry inhibiting properties, and nucleoside reverse transcriptase inhibitors (NRTIs) (3'-azido-2',3'-dideoxythymidine (AZT), 3'-fluoro2',3'-dideoxythymidine (FLT), or 2',3'-dideoxy-3'-thiacytidine (3TC)) were designed to simultaneously provide contraceptive and anti-HIV activity. Two linkers, acetate and succinate, were used to conjugate the nucleoside analogs with CS. The conjugates containing cellulose sulfate-acetate (CSA) (e.g., AZT-CSA and FLT-CSA) were found to be more potent than CS and other conjugates (e.g., AZT-succinate-CS, and FLT-succinate-CS). The presence of both sulfate and the acetate groups on cellulose were critical for generating maximum anti-HIV activity. In addition to showing equal potency against wild-type and multidrug resistant HIV-1, the AZT-CSA conjugate displayed significant contraceptive activity in an animal model, providing the initial proof-of-concept for the design and synthesis of dual-activity compounds based on these combinations. ~1 Citing
104. Synthesis and evaluation of 3-phenylpyrazolo[3,4-d]pyrimidine-peptide conjugates as Src kinase inhibitors By Kumar Anil; Wang Yuehao; Lin Xiaofeng; Sun Gongqin; Parang Keykavous From ChemMedChem (2007), 2(9), 1346-60, Language: English, Database: MEDLINE 3-Phenylpyrazolo[3,4-d]pyrimidine (PhPP) derivatives substituted with an alkyl or aryl carboxylic acid at the N1endocyclic amine, such as PhPP-CH(2)COOH (IC(50)=250 microM), and peptides Ac-CIYKYY (IC(50)=400 microM) and Ac-YIYGSFK (IC(50)=570 microM) were weak inhibitors of polyE(4)Y phosphorylation by active c-Src. A series of PhPP-peptide conjugates were synthesized using PhPP as an ATP mimic and CIYKYY or YIYGSFK as a peptide substrate to improve the inhibitory potency against active c-Src kinase. PhPP derivatives were attached to the N terminus or the side chain of amino acids in the peptide template. Two N-terminal substituted conjugates, PhPPCH(2)CO-CIYKYY (IC(50)=0.38 microM) and PhPP-CH(2)CO-YIYGSFK (IC(50)=2.7 microM), inhibited the polyE(4)Y phosphorylation by active c-Src significantly higher than that of the parent compounds. The conjugation of PhPP with the peptides produced a synergistic inhibition effect possibly through creation of favorable interactions between the conjugate and the kinase domain as shown by molecular modeling studies. ~0 Citings
105. Synthesis and evaluation of tripodal peptide analogues for cellular delivery of phosphopeptides By Ye Guofeng; Nam Nguyen-Hai; Kumar Anil; Saleh Ali; Shenoy Dinesh B; Amiji Mansoor M; Lin Xiaofeng; Sun
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Gongqin; Parang Keykavous From Journal of medicinal chemistry (2007), 50(15), 3604-17, Language: English, Database: MEDLINE Tripodal peptide analogues were designed on the basis of the phosphotyrosine binding pocket of the Src SH2 domain and assayed for their ability to bind to fluorescein-labeled phosphopeptides. Fluorescence polarization assays showed that a number of amphipathic linear peptide analogues (LPAs), such as LPA4, bind to fluorescein-labeled GpYEEI (F-GpYEEI). LPA4 was evaluated for potential application in cellular delivery of phosphopeptides. Fluorescence microimaging cellular uptake studies with fluorescein-attached LPA4 (F-LPA4) alone or with the mixture of LPA4 and F-GpYEEI in BT-20 cells showed dramatic increase of the fluorescence intensity in cytosol of cells, indicating that LPA4 can function as a delivery tool of F-GpYEEI across the cell membrane. Fluorescent flow cytometry studies showed the cellular uptake of F-LPA4 in an energy-independent pathway and confirmed the cellular uptake of F-GpYEEI in the presence of LPA4. These studies suggest that amphipathic tripodal peptide analogues, such as LPA4, can be used for cellular delivery of phosphopeptides. ~0 Citings
106. Design and evaluation of hydroxamate derivatives as metal-mediated inhibitors of a protein tyrosine kinase By Gu Xianfeng; Wang Yuehao; Kumar Anil; Ye Guofeng; Parang Keykavous; Sun Gongqin From Journal of medicinal chemistry (2006), 49(25), 7532-9, Language: English, Database: MEDLINE Protein tyrosine kinases use two Mg(2+) ions as cofactors in catalysis, one as the ATP-Mg complex (M1) and the other as an essential activator (M2). The M2-binding site has high affinity for transition metal cations such as cobalt and zinc. Taking advantage of this high affinity, we examined hydroxamates as metal-mediated inhibitors against Cterminal Src kinase (Csk), a protein tyrosine kinase. Of a small group of amino acid hydroxamates, tyrosine and phenylalanine hydroxamates inhibited Csk activity only in the presence of Co(2+). Four classes of phenylalanine and tyrosine hydroxamate derivatives were synthesized and evaluated as metal-mediated inhibitors of Csk, leading to improved inhibition and a better understanding of the structure-activity relationships. This study suggests that hydroxamates may serve as a general scaffold for developing metal-mediated inhibitors against protein tyrosine kinases. To the best of our knowledge, this is the first report of designing metal-mediated inhibitors against a protein tyrosine kinase by targeting a metal binding site. ~0 Citings
107. Synthesis of polymer-bound 4-acetoxy-3-phenylbenzaldehyde derivatives: applications in solid-phase organic synthesis By Kumar Anil; Ye Guofeng; Ahmadibeni Yousef; Parang Keykavous From The Journal of organic chemistry (2006), 71(20), 7915-8, Language: English, Database: MEDLINE Aminomethyl polystyrene resin was reacted with 4-(5'-formyl-2'-hydroxyphenyl)benzoic acid and 4-(5'-formyl-2'hydroxyphenyl)phenyl propionic acid, respectively, in the presence of 1-hydroxybenzotriazole and 1,3diisopropylcarbodiimide to yield polymer-bound benzaldehydes. The phenolic group in resins was acetylated with acetic anhydride to afford two polymer-bound 4-acetoxybenzaldehydes. The reductive amination of polymer-bound linkers by amines and sodium triacetoxyborohydride, followed by sulfonylation with arylsulfonyl chloride derivatives in
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the presence of pyridine and the cleavage with TFA/DCM/H2O, produced pure sulfonamides. ~1 Citing
108. Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors By Kumar Anil; Ye Guofeng; Wang Yuehao; Lin Xiaofeng; Sun Gongqin; Parang Keykavous From Journal of medicinal chemistry (2006), 49(11), 3395-401, Language: English, Database: MEDLINE A series of peptide analogues of Ac-CIYKYY (1) were synthesized by functional group modifications in peptide side chains or by introducing conformational constraints, to improve the inhibitory potency against active Src kinase. AcCIYKF(4-NO2)Y (2, IC50 = 0.53 microM) and conformationally constrained peptide 31 (IC50 = 0.28 microM) exhibited 750- and 1400-fold higher inhibitory activities, respectively, versus that of 1 (IC50 = 400 microM). Compound 2 exhibited a partial competitive inhibition pattern against ATP. ~1 Citing
109. Biomimetic oxidation of curcumin with hydrogen peroxide catalyzed by 5,10,15,20-tetraarylporphyrinatoiron(III) chlorides in dichloromethane By Chauhan Shive Murat Singh; Kandadai Appan Srinivas; Jain Nidhi; Kumar Anil From Chemical & pharmaceutical bulletin (2003), 51(11), 1345-7, Language: English, Database: MEDLINE The biomimetic oxidation of curcumin, a main turmeric pigment with hydrogen peroxide catalyzed by different 5,10,15,20-tetraarylporphyrinatoiron(III) chlorides [TAPFe(III)Cl] in dichloromethane has been studied to give a C-C coupled curcumin dimer in 40-70% yield. The structure of the dimer has been elucidated by (1)H-, (13)C-NMR, IR and FAB-Mass spectroscopic data. ~0 Citings
110. Biomimetic reduction of nimesulide with NaBH4 catalyzed by metalloporphyrins By Chauhan Shive Murat Singh; Kandadai Srinivas Appan; Kumar Anil From Chemical & pharmaceutical bulletin (2002), 50(10), 1421-2, Language: English, Database: MEDLINE The biomimetic reduction of anti-inflammatory drug, nimesulide (1) with sodium borohydride catalyzed by 5,10,15,20tetraarylporphyrinatoiron(III) chlorides [TAPFe(III)Cl] has been studied in organic solvents under anaerobic and aerobic conditions. ~0 Citings
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