Drug Discovery Group

 

Recent publications since 2000

191.          Chun, B. K.; Olgen, S. Hon, J. H.; Newton, M. G.; Chu, C. K. Enantiomeric Syntheses of Conformationally Restricted D- and L-2’,3’ –endo-methylene Nucleosides from Carbohydrate Chiral Templates. J. Org. Chem. 2000, 65, 685-693.

192.          Pierra, C.; Olgen, S.; Cavalcanti, S. C. H..; Chent, Y-C; Schinazi, R. F.; Chu, C. K. Synthesis and antiviral activities of enantiomeric 1-[2-(hydroxymethyl) cyclopropyl] methyl nucleosides. Nucleosides, Nucleotides & Nucleic Acids. 2000, 19, 253-268.

193.          Copperwood, J. S.; Boyd, V.; Gumina, G.’ Chu, C. K. Synthesis of L=3’-hydroxymethylribonucleosides. Nucleosides, Nucleotides &Nucleic Acids. 2000, 19, 219-236.

194.          Tan, X.; Boudinot, F. D.; Chu, C. K.; Egron, D.; Perigaud, C.; Gosselin, G.; Imbach, J-L; pharmacokinetics of bis((t-butyl-SATE)-AZTMP, a bispivaloythoethyl prodrug for intracellular delivery of zidovudine monophosphate, in mice. Antiviral Chem. & Chemother.. 2000, 11, 203-12.

195.          Bazmi, H. Z.; Hammond, J. L.; Cavalcanti, S. C. H.; Chu, C. K.; Schinazi, R. F.; Mellors, J. W. In vitro selection of mutations in human immunodeficiency virus type 1 reverse transcriptase that decrease susceptibility to (-)-b-D-dioxolane-guanosine and suppress resistance to 3’ –azido-3’- deoxythymidine. Antimicrobial Agents & Chemother.. 2000, 44, 1783-1788.

196.          Gumina, G.; Chong, Y.; Choi, Y.; Chu, C. K. Steroselective Synthesis of Carbocyclic L-4’-Fluoro-2’,3’–dideoxyadenosine. Org. Lett.. 2000, 2, 1229-1231.

197.          Choi, Y.; Li, L.; Grill, S.; Gullen, W.; Lee, C. S.; Gumina, G.; Tsujii, E.; Cheng, Y-C;, Chu, C. K. Structure-activity relationships of (E)-5-(2-bromovinyl)uracil and related pyrimidine nucleosides as antiviral agents for herpes viruses. J. Med. Chem.. 2000, 43, 2538-2546.

198.          Hong, J. H.; Gao, M-Y; Choi, Y.; Cheng, Y-C; Schinazi, R. F.; Chu, C. K. Synthesis of novel 3’-C-methyl-apionucleosides: as asymmetric construction of a quaternary carbon by Claisen rearrangement. Carbohydrate Res. 2000, 328, 37-48.

199.          Chun, B.K.; Schinazi, R. F.; Cheng, Y.-C.; Chu, C. K. Synthesis of 2’,3’-Dideoxy-3’-fluoro-L-ribonucleosides as potential antiviral agents from D-Sorbitol. Carbohydrate Res. 2000, 328, 49-59.

200.          Chu, C. K.; Ma, L.; Olgen, S.; Pierra, C.; Du, J.; Gumina, G.; Gullen, E.; Cheng, Y-C.; Schinazi, R. F. Synthesis and Antiviral Activity of Oxaselenolane Nucleosides. J. Med. Chem., 2000, 43, 3906-3912. 

201.          Li, L.; Dutschman, G.; Gullen, E.; Tsujii, E.; Grill, S.; Choi, Y. S.; Chu, C. K.; Cheng, Y. -C. Metabolism and Mode of Inhibition of Varicella-Zoster Virus by L-b-5-Bromovinyl- (2-hydroxymethyl)-(1,3-dioxolanyl)uracil Is Dependent on Viral Thymidine Kinase. Mol. Pharmacol 2000, 58, 1109-1114. 

202.          Kira, T.; Grill, S .P.; Dutschman, G. E.; Lin, J-S. Qu, F.; Choi, Y. S.; Chu, C. K.; Cheng, Y.-C. Anti-Epstein-Barr Virus (EBV) Activity of b-L-5-Iododioxolane Uracil Is Dependent on EBV Thymidine Kinase. Antimicrobial Agents & Chemother. 2000, 44, 3278-3284.

203.          Chong, Y.; Gumina, G.; Chu, C. K. Divergent Synthesis of D- and L- Carbocyclic 4’-Fluoro-2’, 3’-Dideoxynucleosides as Potential Antiviral Agents. Tetrahedron: Asymm. 2000, 11, 4853-4875.

204.          Furman, P. A.; Jeffrey, J.; Kiefer, L. L.; Feng, J.; Anderson, K. S.; Borrota-Esoda, K.; Hill, E.; Copeland, W. C.; Chu, C. K.; Sommadossi, J. P.; Liberman, I.; Schinazi, R. F.; Painter, G. R. A mechanism of Action of 1-b-D-2, 6-Diaminopurine Dioxolane: A Prodrug of the human immunodeficiency virus1 Inhibitor 1-b-D-Dioxolane Guanosine. Antimicrobial Agents & Chemother. 2001, 45, 158-165. 

205.          Lee, K.; Chu, C. K. Understanding the Mode of Action of L-Nucleosides as Antiviral Agents: A Molecular Modeling Approach. Antimicrob. Agents Chemother. 2001, 45, 138-144.

206.          Cho, S.; Kim, Y.; Cruz, M .O.; Park, E. -M.; Chu, C. K.; Lee, K.; Joh, T. H. Repression of proinflammatory cytokine and inducible oxide syntheses (NOS2) gene expression in activated microglia by N-acetyl-O-methyldopamine: Protein kinase A-dependent mechanism. Glia. 2001, 33, 324-333.

207.          Chun, B. K.; Song, G. Y.; Chu, C .K. Stereocontrolled Syntheses of Carbocyclic C-Nucleosides and Related Compounds. J. Org. Chem., 2001, 66, 4852-4858. 

208.          Gumina, G.; Song, G .Y.; Chu, C. K. Advances in Antiviral Agents for Hepatitis B Virus. - Antiviral Chem. Chemother., 2001, 12, 89-112. 

209.          Korba, B. E.; Cote, P.; Baldwin, B. H.; Wells, F. V.; Peek, S. F.; Hornbuckle, W. E.; Toshkov, I. A.; Chu, C. K.; Gerin, J. L.; Tennant, C. B. C.; Jacob, J. R. Antiviral Activity of clevudine [L-FMAU, (1-(2-fluoro-5-methyl-beta, 1-arabinofuranosyl) uracil)] against woodchuck hepatitis virus replication and gene expression in chronically infected woodchucks (Marmota monax). Hepatology, 2001, 33, 254-266. 

210.          Choo, H.; Chong, Y. H.; Chu, C. K. Solid Phase Synthesis of Carbocyclic L-2’-Deoxynucleosides, Org. Lett., 2001, 3, 1471-1473. 

211.          Clark, T. N.; White, C. A.; Chu, C. K.; Bartlett, M .G. Determination of 3’-azido-2, 3’-dideoxyridine in maternal Plasma, Amniotic Fluid, Fetal and Placental Tissues by High Performance Liquid Chromatography, J. of Chromatography B, 2001, 755,165-172. 

212.          Gumina, G.; Song, G. Y.; Chu, C. K. L-Nucleosides as chemotherapeutic. FEMS Microbiol. Lett., 2001, 202, 9-15. 

213.          Gumina, G.; Schinazi, R. F.; Chu, C. K. Synthesis and potent anti-HIV activity of L-3’-fluoro 2’, 3’-unsaturated cytidine, Org. Lett., 2001, 3, 4177-4180. 

214.          Song, G. Y.; Paul, V.; Choo, H.; Morrey, J.; Sidwell, R. W.; Schinazi, R. F.; Chu, C. K. Enantiomeric Synthesis of D- and L-Cyclopentenyl Nucleosides and their Antiviral Activity Against HIV and West Nile Virus, J. Med. Chem., 2001, 44, 3985-3993.

215.          Song, G. Y.; Naguib, F. N. M.; El Kouni, M.; Chu, C. K. Synthesis of carbocyclic orotidine analogs as potential orotidine decarboxylase inhibitors, Nucleosides, Nucleotides & Nucleic Acids, 2002, 20, 1915-1925. 

216.          Lee, K.; Choi, Y. S.; Gumina, G.; Zhou, W.; Schinazi, R. F.; Chu, C. K. Structure-Activity Relationships of 2’-Fluoro-2’, 3’-unsaturated D-Nucleosides as Anti-HIV-1 Agents. J. Med. Chem., 2002, 45, 1313-1320.

217.          Chong, Y. H.; Chu, C. K. Efficient synthesis of 2-deoxy-L-erythro-pentose (2-deoxy-L-ribose) from l-arabinose. Carbohydrate Res., 2002, 332, 397-402.

218.          Choi, Y. S.; Choo, H.; Chong, Y.; Lee, S.; Olgen, S.; Schinazi, R. F.; Chu, C. K. Synthesis and Potent Anti-HIV Activity of L-2’,3’-Didehydro-2’,3’-dideoxy-2’-fluoro-4’-thiocytidine. Org. Lett., 2002, 4, 305-307. 

219.          Ray, A. S.; Yang, Z.; Chu, C. K.; Anderson, K. S. Novel Use of a guanosine prodrug approach to convert 2’, 3’ –didehydro-2’, 3’-dideoxguanosine into a viable Antiviral Agent. Antimicrobial Agents and Chemother., 2002, 46, 887-891. 

220.          Cooperwood, J .S.; Gumina, G.; Vorobiev, A.; Boudinot,F. D.; Chu, C.K. Nucleoside Prodrugs- Recent Advances in Nucleoside: Chemistry and Chemotherapy, C. K. Chu Ed., 2002, Elsevier. 

221.          Gumina, G.; Chu, C. K. Synthesis of L-Oxetanocin, Org. Lett., 2002, 4, 1147-1149.

222.          Jin, Y. H.; Chu, C. K. Efficient and practical synthesis of D-cyclopent-2-enone, the key intermediate for the synthesis of carbocyclic nucleosides, Tet.Lett. 2002, 43, 4141-4143. 

223.          Ray, A. S.; Yang, Z. J.; Shi, J.; Hobbs, A.; Schinazi, R. F.; Chu, C. K.; Anderson, K. S. Insights into the molecular mechanism of inhibition and drug resistance of HIV-1 RT with carbovir triphosphate, Biochemistry, 2002, 41, 5150-5162. 

224.          Gumina, G.; Chong, Y. H.; Choo, H.; Song, G. Y.; Chu, C. K. L-Nucleosides: antiviral activity and molecular mechanism. Current Topics in Med. Chem. 2002, 2, 1065-1086. 

225.          Lee, K.; Zhou, W.; Kelley, L. C.; Momany, C.; Chu, C. K. Synthesis of unsaturated floride containing D- and L-pyranosyl nucleosides. Tet. Asymm. 2002, 13, 1589-1598. 

226.          Chong, Y. H.; Chu, C. K. Understanding the unique mechanism of L-FMAU (clevudine) against heparitis B virus: molecular dynamics studies. Bioorg. Med. Chem. Letts. 2002, 12, 3459-3462. 

227.          Chong, Y.; Borroto-Esoda, K.; Furman, P. A.; Schinazi, R. F.; Chu, C. K. Molecular mechanisms of DAPD/DXG against zidovudine- and lamivudine- drug resistance drug resitant mutant: A molecular modeling approach, Antimicrob. Chemistry Chemother. 2002, 13, 115-128. 

228.          Stuyver, L. J.; Lostia, S.; Adams, M.; Mathew, J. S.; Pai, B. S.; Grier, J. P.; Tarnish, P. M.; Choi, Y. S.; Chong, Y. H.; Choo, H. Chu, C. K.; Otto, M .J.; Schinazi, R. F. Antiviral activity and cellular toxicity of 2’, 3’-dideoxy-2’,3’-didehydrocytidine- analogs,- Antimicrob. Agents. Chemother. 2002, 46, 3854-3860.

229.          Chu, C. K.; Jin, Y. H.; Baker, R. O.; Huggins, J. Antiviral Activity of Cyclopentenyl nucleosides against Orthopox viruses (Smallpox, Monkeypox and Cowpox), Bioorg. Med. Chem. Lett., 2002, 13, 9-11.

230.          Chong, Y. H.; Choo, H. A.; Choi, Y .S.; Schinazi, R. F.; Chu, C. K. Stereoselective synthesis and antiviral activity of D-2’,3’-didehydro-2’,3’-2’-fluoro-4’-thionucleosides, J. Med. Chem., 2002, 45, 4888-4898.

231.          Stuyver, L.J.; Whitaker, McBrayer, T.R.; Hrtnandez, B.I.; Lostia, S. ; Tarnish, P.M. Ramesh, M.; Chu, C. K.; Shi, J.; Jordan, R.; Watnabe, K. A.; Rachakonda, S.; Otto, M. J.; Schnazi, R. F. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture, Antimicrob. Agents. Chemother., 2003, 47, 244-254.

232.          Choo, H. A.; Chong, Y. H.; Choi, Y .S.; Mathew, J.; Schinazi, R .F; Chu, C. K. Synthesis, anti-HIV activity and molecular mechanism of drug resistance of L-2’, 3’-didehydro-2, 3’-dideoxy-2’-fluoro-4’-thionucleosides, J. Med. Chem., 2003, 46, 389-398. 

233.          Chen, H.; Pai, B.; Hurwitz, S .J.; Chu, C. K.; Glazkova, Y.; MaClure, H. M.; Feitelstein, M.; Schinazi, R. F. Antiviral activity and pharmacokinetics of 1-(2,3-dideoxy-2-fluoro-β-L-glyceropent-2-enofuranosyl)cytosine, Antimicrob. Agents Chemother., 2003, 47, 1922-1928. 

234.          Choo, H. A.; Chong, Y .H.; Chu, C. K. The Role of 2’, 3’-unsaturation on the antiviral activity of anti-HIV nucleosides against #TC-resistant mutant (M184V). Bioorg. Med. Chem. Lett., 2003,13, 1993-1996. 

235.          Chong, Y .H.; Gumina, G.; Mathew, J.; Schinazi, R .F.; Chu, C. K. L-2’, 3’-Dihydro-2’,3’-dideoxy-3’-fluoronucleosides: Synthesis, anti-HIV activity, chemical and enzymatic stability amd the mechanism of resistance, J. Med. Chem. 2003, 46, 3245-3256. 

236.          Zhu, W.; Gumina, G.; Schinazi, R. F.; Chu, C. K. Synthesis and anti-HIV activity of L-b-3’-C-cyano-2’,3’-unsaturated nucleosides and L-3’-C-cyano-3’-deoxyribonucleosides, Tetrahedron 2003, 59, 6423-6431. 

237.          Jin, Y. H.; Liu, P.; Chu, C. K. Practical synthesis of D- & L-cyclopent-2,3-none and their utility for the synthesis of carbocyclic antiviral nucleosides against orthopox viruses (smallpox, Monkeypox and cowpoxvirus), J. Org. Chem. 2003, 68, 9012-9018. 

238.          Chong, Y. H.; Akula, N.; Chu, C. K. Studies of molecular mechanism of Tenofovir against 3TC- and AZT-resistance mutant HIV-1 reverse transcriptase, Bioorg. Med. Chem. Letts. 2003, 13, 4019-4022. 

239.          Ray, A. S.; Schinazi, R. F. Murakami, E.; Basavpthruni, A.; Shi, J.; Zorea, S.; Schinazi, R. F.; Chu, C. K.; Anderson, K. S. Probing the mechanistic consequences of 5-fluoro substitution on cytidine nucleotide analogs incorporation by HIV-1 reverse transcriptase, Antiviral Chem. Chemother. 2003, 14, 115-125. 

240.          Kong, L.; Cooperwood, J,; Huang, C.; Chu, C. K.; Boudinot, F. D. Pharmacokinetic evaluation of 3'-azido-2', 3'-dideoxyuridine-5'-O-valinate-hydrochloride as a prodrug of the anti-HIV nucleoside 3'-azido-2', 3'-dideoxyuridine, Antimicrob. Chem. Chemother. 2003, 14, 263-270. 

241.          Kong, Linghui, Cooperwood, John S., Oh, Chang H., Chu, Chung K.; Boudinot, F. Douglas. Simultaneous determination of 3’-azido-2’, 3’-dideoxyuridine and novel prodrugs in rat plasma by liquid chromatography._ Journal of Chromatography B 2003, 795, 371-376. 

242.          Stuyver, L.; McBrayer, T . R.; Tharnish, P. M.; Hassan, A. E. A.; Chu, C. K.; Pankiewicz, K. W.; Watanabe, K. A.; Schinazi, R. F.; Otto, M. J. Dynamics of subgenomic hepatitis C replicon RNA levels in Huh7 cells after exposure to nucleoside antimetabolites, J. Virology, 2003, 77, 10689-10694.

243.          Chong, Y.H.; Stuyver, L.; Otto, M.J.; Schinazi, R.F.; Chu, C. K. Mechanism of antiviral activities of 3’-substituted L-nucleosides against 3TC-resistant HBV polymerase: a molecular modeling approach. Antiviral Chem. Chemother. 2003, 14, 309-319.

244.          Chong, Y. H.; Chu, C. K. Understanding the molecular mechanism of drug resistance of anti-HIV nucleosides by molecular modeling, Frontiers in Bioscience, 2004, 9, 164-186.

245.          Chong, Y. H.; Choo, H .A.; Chu, C. K. Effects of fluorine substitution of cytosine analogs on the binding affinity to HIV-1 reserse transcriptase, Bioorg. Med. Chem. Lett. 2004, 14, 437-440.

246.          Park, E. M.; Joh, T. H.; Volpe, B .T.; Chu, C. K.; Song, G.; Cho, S. A neuroprotective role of extracellular signal-regulated kinase in n-acethyl-o-methyldopamine-treated hippocampal neurons after exposure to in vitro and in vivo ischemia, Neuroscience, 2004, 123, 147-154.

247.          Song, J. Wang, X-L.; Xiang, Y-J; Chu, C. K.; Schinazi, R. F.; Zhao, K. Synthesis of b-L-2', 3'-Dideoxy-2'-Fluoro-3'-hydroxymethylarabinofuranosyl Pyrimidine nucleosides, Chinese Chem. Lett, 2004, 15, 135-7. 

248.          Zhu, W.; Chong, Y. H.; Choo, H.; Mathews, J.; Schinazi, R. F.; Chu, C. K. Synthesis, structure-activity relationships, Mechanism of Drug Resistance of D-and- L-b-3’-Fluoro-2’, 3’-unsaturated-4-thioucleosidesas anti-HIV Agents. J. Med. Chem.- 2004, 47, 1631-1640. 

249.          Shi, J. X.; Ray, A. S.; Mathew, J. S.; Anderson, K. S.; Chu, C. K.; Schinazi, R. F. 2’, 3’-Didehydro-2’, 3’-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions, Bioorg. Med. Chem. Lett, 2004, 14, 2159-2162.

250.          Chong, Y. H.; Chu, C. K. Molecular mechanism of dioxolane nucleosides against 3TC resistant M184 mutant HIV. Antiviral Res. 2004, 63, 7-13. 

251.          Yadav, V.; Rais, R.; Naguib, F. N. M.; el Kouni, M.; Chu, C. K. Synthesis, Biological Activity and Molecular modeling of 6-Benzylthioinosien analogs as subversive Substrates of Toxoplasma gondii Adenosine Kinase. J. Med. Chem. 2004, 47, 1987-1996. 

252.          Hollecker, L.; Lostia, S.; McBrayer, T. R.; Chu, C. K. Stuyver, L. J.; Rachakonda, S.; Shi, J.; Watanabe, K. A. Synthesis of b-enantiomers of N4-hydroxy-3’-deoxypyrimidine nucleosides and their evaluation against bovine viral diarrhoea virus and hepatitis C virus in cell culture, Antiviral Chem. Chemother. 2004, 15, 43-55.

253.          Zhou, W.; Gumina, G.; Chong, Y. H.; Wang, J.; Schinazi, R. F.; Chu, C. K. Synthesis, structure-activity relationships and drug resistance of D-3’-fluoro-2’, 3’ -unsaturated nucleosides as anti-HIV agents, J. Med. Chem. 2004, 47, 3399-3408.

254.          Bondada, L.; Gumina, G.; Nair, R.; Ning, X. H.; Chu, C. K. Synthesis of novel spiro [2.3] hexane carbocyclic nucleosides via enzymatic resolution, Org. Lett. 2004, 6, 2531-2534. 

255.          Yadav, V.; Chu, C. K. Molecular mechanism of adefovir sensitivity and resistance in HBV polymerase mutants: a molecular dynamic study, Bioorg. Med. Chem. Lett.. 2004, 14, 4313-4317. 

256.          Hernandez-Santiago, B. I.; Beltran, T.; Stuyver, L.; Chu, C. K.; Schinazi, R. F. Metabolism of the anti-hepatitis C virus nucleoside b-D-N4-hydroxycytidine in different liver cells. Antimicrob. Agents. Chemother. 2004, 48, 4636-4642.

257.          Chen, X.; Zhou, W.; Schinazi, R .F.; Chu, C. K. Synthesis of 3’-Fluoro-2’, 3’-didehydro-4’-ethynyl D- & L-furanosyl-nucleosides, J. Org. Chem. 2004, 69, 6034-6041.

258.          Asif, G.; Hurwitz, S. J.; Gumina, G.; Chu, C. K.; McClure, H. M.; Schinazi, R. F. Pharmacokinetics of the antiviral agent b-L-3’-fluoro- 2’, 3’-didehydro-2’,3’–dideoxycytidine in rhesus monkeys. Antimicrobial Agents & Chemother.. 2005, 49, 560-564.

259.          Shi, J.; Du, J.; Ma, T.; Pankiewicz, K. W.; Patterson, S. E.; Tharnish, P. M.; McBrayer, T. R.; Stuyver, L. J.; Otto, M. J.; Chu, C. K.; Schinazi, R. F.; Watanabe, K. A. Synthesis and anti-viral activity of a series of D- and L-2’ –fluroribonucleosides in the subgenomic HCV replicon system. Bioorg. Med. Chem.. 2005, 13, 1641-1652.

260.          Shi, J,; Du, J.; Ma, T.; Pankiewicz, K. E.; Patterson, S. E.; Hassan, A. E. A.; Tharnish, P. M.; McBrayer, T. R.; Lostia, S. Stuyver, L. J. ; Wantanabe, K. A.; Chu, C. K.; Schinazi, R. F. Synthesis and in vitro antti-HCV activity of b-D and L-2;-deoxy-2;-fluororibonucleosides. Nucleosides, Nucleotides, & Nucleic Acids. 2005, 24, 875-879.

261.          Choo, H. A. Chong, Y. H.; Gumina, G.; Chu, C. K. Advances in antiviral nucleosides in Frontiers in Nucleosides and Nucleic Acid, Schinazi and Liotta (Edition), IHL Press,  2005, 101-158.

262.          Ray, A. S.; Hernandez-Santiago, B. I.; Mathew, J. S.; Murakami, E.; Bozeman, C.; Xie, M-Y,; Dutchman, G. E.; Gullen, E.; Yang, Zhenjun, H.; Hurwitz, S.; Cheng, Y-C,; Chu, C. K.; McClure, H.; Schinazi, R. F.; Anderson, K. S. Mechanism of anti-human immunodeficiency virus activity of b-D-6-cyclopropylamin – 2’, 3’-dideoxyguanosine. Antimicrobial Agents & Chemother.. 2005, 49, 1994-2001.

263.          Wang, P.Y.; Adams, M.; Grier, J.P.;Pai, B.; Mathew, J.; Watanabe, K.A.; Otto, M. J.; Gumina, G.; Chu, C. K. ; Schinazi, R.F. Synthesis and in vitro anti-HIV activity of 2’-fluoro-2’,3’-didehydro-2’,3’-dideoxypurine nucleosides in Frontiers in Nucleosides and Nucleic Acid, Schinazi and Liotta (Edition), IHL Press,  2005, 227-234.

264.          Rais, R. H.; Al Safarjalani, O. N.; Yadav, V.; Guarcello, N.; Kirk, M.; Chu, C. K.; Naguib, F. N. M.; El Kouni, M. H. 6-Benzylthionosine analogues as subversive substrate of Toxoplasma gondii adenosine kinase: activities and selective toxicities. Biochem. Pharmacol. 2005, 69, 1409-1419.

265.          Wang, J.; Jin, Y.; Rapp, K. L.; Bennett, M.; Schinazi, R. F.; Chu, C. K. Synthesis, antiviral Activity, and Mechanism of Drug Resistance of D- and L-2’,3’-Didehydro-2’,3,- dideoxy-2;- fluorocarbocyclic, Nucleosides. J. Med. Chem. 2005, 48, 3736-3748.

266.          Chu, C. K.; Yadav, V.; Chong, Y.H.; Schinazi, R.F. (-)-(2R, 4R)-(2-Hydroxymethyl-1,3-dioxolan-4-yl)thymine (Dioxolane-thymine or DOT) against drug resistant HIV-1 mutants and its molecular mechanism. J. Med. Chem. 2005, 48, 3949-3952.

267.          Hernandez-Santiago, B. I., Chen, H.; Asif, G.; Beltran, T.; Mao, S. J.; Grier, J.; McClure, H. M.; Chu, C. K.; Liotta, D. C.; Schinazi, R. F. Pharmacology and pharmacokinetics of the antiviral agent b-D-2;'3'-dideoxy-3; - oxa-5-fluorocytidine in cells and rhesus monkeys. Antimicrobial Agents & Chemother.. 2005, 49, 2589-2597.

268.          Choi, S.R.; Zhung, Z.P.; Acton, P.D.; Tjuvajev-Gelovani, J.; Doubrovin, M.; Chu, C. K.; Kung, H.F. SPECT imaging of herpes simplex virus type 1 thymidine kinase gene expression by [123I]FIAU, Academic Radiology 2005, 12, 798-805.

269.          Hammond, J. L.; Parikh, U. M.; Koontz, D. L.; Schlueter-Wirtz, S.; Chu, C. K.; Bazmi, Hengameh, A.; Schinazi, R. F.; Mellors, J. W. In vitro selection and analysis of humone immunodeficiency virus type 1 resistant to derivatives of b-2’, 3’ -dideoxy-5-fluorocytidine. Antimicrobial Agents & Chemother.. 2005, 49, 3930-3932.

270.          Casey, J.; cote, P. J.; Toshkov, I. A.; Chu, C. K.; Gerin, J. L.; Hornbuckle, W. E.; Tennant, B. C.; Korba, B. E. Clevudine inhibits hepatitis delta virus viremia: A pilot study of chronically infected woodchucks. Antimicrobial Agents & Chemother.. 2005, 24, 4396-4399.

271.          Gupte, A.; Buolamwini, J. k.; Yadav, V.; Chu, C. K.; Naguib, F. N. M.; el Kouni, M. H. 6-Benzylthionsine analogues: Promising anti-toxoplasmic agents as inhibitors of the mammalian nucleoside transporter ENT1(es). Biochem. Pharmacol. 2005, 71, 69-73

272.          Gumina, G.; Chu, C. K. L-Nucleosides as chemotherapeutic agents, Book chapter,  2005, in press.

273.          Pai, S. B.; Pai, T. B.; Xie, M-Y; Beker, T.; Shi, J.; Tharnish, P. M.; Chun, C. K.; Schinazi, R. F. Characterization of hepatitis B virus inhbiton by novel 2’-fluoro-2’,3’-unsaturated beta-D- and L-nucleosides. Antiviral Chem. & Chemother. 2005, 16, 183-192.

274.          Gadthula, S.; Schinazi, R.F.; Chu, C. K. Synthesis and anti-HIV activity of β-D-3’-azido-2'3'-unsaturated nucleosides and β-D-3’-azido-3’-deoxyribofuranosylnucleosides, Nucleosides, Nuceotides, and Nucleic Acids, 2005, 24, 1707-1727

275.          Choo, H.; Chen, X.; Yadav, V.; Wang, J.; Schinazi, R. F.; Chu, C. K. Synthesis and Anti-HIV Activity of D- and L-Thietanose Nucleosides. J. Med. Chem.. 2006, 49, 1635-1647.

276.          Cho, J. H.; Bernard, D. L.; Sidwell, R. W.; Kern, E. R.; Chu, C. K. Synthesis of cyclopentenyl carbocyclic nucleosides as potential antiviral agents against orthopoxviruses and SARS. J. Med. Chem. 2006, 49, 1140-1148.

277.          Liang, Y.; Narayanasamy, J. Schinazi, R. F.; Chu, C. K. Phosporamidate and phosphate prodrugs of (-)-b-D- (2R, 4R)-dioxolane-tymine: synthesis, anti-HIV activity and stability studies. Bioorg. Med. Chem.. 2006, 14, 2178-2189.

278.          Arumugham, B.; Kim, H-J; Prichard, M. N.; Kern, E. R.; Chu, C. K. Synthesis and antiviral activity of 7-deazaneplanocia A against orthopoxviruses (vaccinia and cowpox virus). Bioorg. Med. Chem. Lett.. 2006, 16, 285-281.

279.          Zhang, H.; Schinazi, R. F.; Chu, C. K., Synthesis of neplanocin F analogues as potential antiviral agents. Bioorganic & Medicinal Chemistry 2006, 14, (24), 8314-8322.

280.          Chu, C. K.; Gadthula, S.; Chen, X.; Choo, H.; Olgen, S.; Barnard, D. L.; Sidwell, R. W., Antiviral activity of nucleoside analogues against SARS-coronavirus (SARS-coV). Antivir Chem Chemother 2006, 17, (5), 285-9.

281.          Liu, P.; Chu, C. K., Enantiomeric synthesis of carbocyclic analogs of D-and L-6-azapyrimidine ribonucleosides. Canadian Journal of Chemistry 2006, 84, (4), 748-754.

282.          Liu, P.; Sharon, A.; Chu, C. K., Enantiomeric synthesis of carbocyclic d-4'-C-methylribonucleosides as potential antiviral agents. Tetrahedron: Asymmetry 2006, 17, (23), 3304-3314.

283.          Radi, M.; Adema, A. D.; Daft, J. R.; Cho, J. H.; Hoebe, E. K.; Alexander, L. E.; Peters, G. J.; Chu, C. K., In Vitro Optimization of Non-Small Cell Lung Cancer Activity with Troxacitabine, L-1, 3-Dioxolane-cytidine, Prodrugs. J. Med. Chem 2007, 50, (9), 2249-2253.

284.          Kim, Y. A.; Sharon, A.; Chu, C. K.; Rais, R. H.; Al Safarjalani, O. N.; Naguib, F. N. M.; el Kouni, M. H., Synthesis, biological evaluation and molecular modeling studies of N6-benzyladenosine analogues as potential anti-toxoplasma agents. Biochemical Pharmacology 2007, 73, (10), 1558-1572.

285.          Wang, J.; Jin, Y.; Rapp, K. L.; Schinazi, R. F.; Chu, C. K., D-and L-2', 3'-Didehydro-2', 3'-dideoxy-3'-fluoro-carbocyclic Nucleosides: Synthesis, Anti-HIV Activity and Mechanism of Resistance. J. Med. Chem 2007, 50, (8), 1828-1839.

286.          Narayanasamy, J.; Pullagurla, M. R.; Sharon, A.; Wang, J.; Schinazi, R. F.; Chu, C. K., Synthesis and anti-HIV activity of (-)-ß-d-(2R, 4R)-1, 3-dioxolane-2, 6-diamino purine (DAPD)(amdoxovir) and (-)-ß-d-(2R, 4R)-1, 3-dioxolane guanosine (DXG) prodrugs. Antiviral Research 2007, 75, (3), 198-209.

287.          Asif, G.; Hurwitz, S. J.; Obikhod, A.; Delinsky, D.; Narayanasamy, J.; Chu, C. K.; McClure, H. M.; Schinazi, R. F., Pharmacokinetics of the Anti-Human Immunodeficiency Virus Agent 1-({beta}-D-Dioxolane) Thymine in Rhesus Monkeys. Antimicrobial Agents and Chemotherapy 2007, 51, (7), 2424.

288.          Menne, S.; Asif, G.; Narayanasamy, J.; Butler, S. D.; George, A. L.; Hurwitz, S. J.; Schinazi, R. F.; Chu, C. K.; Cote, P. J.; Gerin, J. L., Antiviral Effect of Orally Administered (-)-ß-d-2-Aminopurine Dioxolane in Woodchucks with Chronic Woodchuck Hepatitis Virus Infection? Antimicrobial Agents and Chemotherapy 2007, 51, (9), 3177-3184.

289.          Rao, J. R.; Schinazi, R. F.; Chu, C. K., Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides. Bioorganic & Medicinal Chemistry 2007, 15, (2), 839-846.

290.          Peng, L.; Sharon, A.; Chu, C. K., Fluorinated Nucleosides: Synthesis and Biological Implication. Journal of Fluorine Chemistry 2008, In Press

291.          Kim, Y. A.; Sharon, A.; Chu, C. K.; Rais, R. H.; Al Safarjalani, O. N.; Naguib, F. N. M.; el Kouni, M. H., Structure-Activity Relationships of 7-Deaza-6-benzylthioinosine Analogues as Ligands of Toxoplasma gondii Adenosine Kinase. J. Med. Chem. 2008. In Press.

 

 


 

 

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Last Update: 06/22/08