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Page 1
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.
Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, Weller PE. Talamas FX, et al. Among authors: leveque v. J Med Chem. 2014 Mar 13;57(5):1914-31. doi: 10.1021/jm401329s. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24195700 Free PMC article.
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. 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
De novo fragment design: a medicinal chemistry approach to fragment-based lead generation.
Talamas FX, Ao-Ieong G, Brameld KA, Chin E, de Vicente J, Dunn JP, Ghate M, Giannetti AM, Harris SF, Labadie SS, Leveque V, Li J, Lui AS, McCaleb KL, Nájera I, Schoenfeld RC, Wang B, Wong A. Talamas FX, et al. Among authors: leveque v. J Med Chem. 2013 Apr 11;56(7):3115-9. doi: 10.1021/jm4002605. Epub 2013 Mar 29. J Med Chem. 2013. PMID: 23509929
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: leveque v. 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.
The design, synthesis, and antiviral activity of monofluoro and difluoro analogues of 4'-azidocytidine against hepatitis C virus replication: the discovery of 4'-azido-2'-deoxy-2'-fluorocytidine and 4'-azido-2'-dideoxy-2',2'-difluorocytidine.
Smith DB, Kalayanov G, Sund C, Winqvist A, Maltseva T, Leveque VJ, Rajyaguru S, Le Pogam S, Najera I, Benkestock K, Zhou XX, Kaiser AC, Maag H, Cammack N, Martin JA, Swallow S, Johansson NG, Klumpp K, Smith M. Smith DB, et al. J Med Chem. 2009 May 14;52(9):2971-8. doi: 10.1021/jm801595c. J Med Chem. 2009. PMID: 19341305
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. 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 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. 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. 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
The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture.
Klumpp K, Lévêque V, Le Pogam S, Ma H, Jiang WR, Kang H, Granycome C, Singer M, Laxton C, Hang JQ, Sarma K, Smith DB, Heindl D, Hobbs CJ, Merrett JH, Symons J, Cammack N, Martin JA, Devos R, Nájera I. Klumpp K, et al. Among authors: leveque v. J Biol Chem. 2006 Feb 17;281(7):3793-9. doi: 10.1074/jbc.M510195200. Epub 2005 Nov 29. J Biol Chem. 2006. PMID: 16316989 Free article.
40 results