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Page 1
Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors.
Antonysamy SS, Aubol B, Blaney J, Browner MF, Giannetti AM, Harris SF, Hébert N, Hendle J, Hopkins S, Jefferson E, Kissinger C, Leveque V, Marciano D, McGee E, Nájera I, Nolan B, Tomimoto M, Torres E, Wright T. Antonysamy SS, et al. Among authors: najera i. Bioorg Med Chem Lett. 2008 May 1;18(9):2990-5. doi: 10.1016/j.bmcl.2008.03.056. Epub 2008 Mar 22. Bioorg Med Chem Lett. 2008. PMID: 18400495
3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase.
Hendricks RT, Spencer SR, Blake JF, Fell JB, Fischer JP, Stengel PJ, Leveque VJ, Lepogam S, Rajyaguru S, Najera I, Josey JA, Swallow S. Hendricks RT, et al. Among authors: najera i. Bioorg Med Chem Lett. 2009 Jan 15;19(2):410-4. doi: 10.1016/j.bmcl.2008.11.060. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19070486
Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors.
Hendricks RT, Fell JB, Blake JF, Fischer JP, Robinson JE, Spencer SR, Stengel PJ, Bernacki AL, Leveque VJ, Le Pogam S, Rajyaguru S, Najera I, Josey JA, Harris JR, Swallow S. Hendricks RT, et al. Among authors: najera i. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3637-41. doi: 10.1016/j.bmcl.2009.04.119. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19447623
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones.
de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Tracy J, Chin E, Li J, Wang B, Bamberg JT, Stephenson R, Oshiro C, Harris SF, Ghate M, Leveque V, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R, Xu B. de Vicente J, et al. Among authors: najera i. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3642-6. doi: 10.1016/j.bmcl.2009.05.004. Epub 2009 May 7. Bioorg Med Chem Lett. 2009. PMID: 19457662
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.
de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Zhao J, Elworthy TR, Tracy J, Chin E, Li J, Lui A, Wang B, Oshiro C, Harris SF, Ghate M, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Fitch B, Brandl M, Masjedizadeh M, Wu SY, de Keczer S, Voronin T. de Vicente J, et al. Among authors: najera i. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5648-51. doi: 10.1016/j.bmcl.2009.08.023. Epub 2009 Aug 8. Bioorg Med Chem Lett. 2009. PMID: 19700319
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.
de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Li J, Wang B, Bamberg JT, Harris SF, Wong A, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R. de Vicente J, et al. Among authors: najera i. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5652-6. doi: 10.1016/j.bmcl.2009.08.022. Epub 2009 Aug 8. Bioorg Med Chem Lett. 2009. PMID: 19709881
Discovery of a novel series of potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Schoenfeld RC, Bourdet DL, Brameld KA, Chin E, de Vicente J, Fung A, Harris SF, Lee EK, Le Pogam S, Leveque V, Li J, Lui AS, Najera I, Rajyaguru S, Sangi M, Steiner S, Talamas FX, Taygerly JP, Zhao J. Schoenfeld RC, et al. Among authors: najera i. J Med Chem. 2013 Oct 24;56(20):8163-82. doi: 10.1021/jm401266k. Epub 2013 Oct 10. J Med Chem. 2013. PMID: 24069953 Free PMC article.
Selection and characterization of replicon variants dually resistant to thumb- and palm-binding nonnucleoside polymerase inhibitors of the hepatitis C virus.
Le Pogam S, Kang H, Harris SF, Leveque V, Giannetti AM, Ali S, Jiang WR, Rajyaguru S, Tavares G, Oshiro C, Hendricks T, Klumpp K, Symons J, Browner MF, Cammack N, Nájera I. Le Pogam S, et al. Among authors: najera i. J Virol. 2006 Jun;80(12):6146-54. doi: 10.1128/JVI.02628-05. J Virol. 2006. PMID: 16731953 Free PMC article.
Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479.
Smith DB, Martin JA, Klumpp K, Baker SJ, Blomgren PA, Devos R, Granycome C, Hang J, Hobbs CJ, Jiang WR, Laxton C, Le Pogam S, Leveque V, Ma H, Maile G, Merrett JH, Pichota A, Sarma K, Smith M, Swallow S, Symons J, Vesey D, Najera I, Cammack N. Smith DB, et al. Among authors: najera i. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6. doi: 10.1016/j.bmcl.2007.02.004. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17317178
Slow binding inhibition and mechanism of resistance of non-nucleoside polymerase inhibitors of hepatitis C virus.
Hang JQ, Yang Y, Harris SF, Leveque V, Whittington HJ, Rajyaguru S, Ao-Ieong G, McCown MF, Wong A, Giannetti AM, Le Pogam S, Talamás F, Cammack N, Nájera I, Klumpp K. Hang JQ, et al. Among authors: najera i. J Biol Chem. 2009 Jun 5;284(23):15517-29. doi: 10.1074/jbc.M808889200. Epub 2009 Feb 26. J Biol Chem. 2009. PMID: 19246450 Free PMC article.
89 results