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Page 1
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: klumpp k. 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
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. 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.
Application of the phosphoramidate ProTide approach to 4'-azidouridine confers sub-micromolar potency versus hepatitis C virus on an inactive nucleoside.
Perrone P, Luoni GM, Kelleher MR, Daverio F, Angell A, Mulready S, Congiatu C, Rajyaguru S, Martin JA, Levêque V, Le Pogam S, Najera I, Klumpp K, Smith DB, McGuigan C. Perrone P, et al. Among authors: klumpp k. J Med Chem. 2007 Apr 19;50(8):1840-9. doi: 10.1021/jm0613370. Epub 2007 Mar 17. J Med Chem. 2007. PMID: 17367121
First example of phosphoramidate approach applied to a 4'-substituted purine nucleoside (4'-azidoadenosine): conversion of an inactive nucleoside to a submicromolar compound versus hepatitis C virus.
Perrone P, Daverio F, Valente R, Rajyaguru S, Martin JA, Lévêque V, Le Pogam S, Najera I, Klumpp K, Smith DB, McGuigan C. Perrone P, et al. Among authors: klumpp k. J Med Chem. 2007 Nov 1;50(22):5463-70. doi: 10.1021/jm070362i. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914786
The design, synthesis, and antiviral activity of 4'-azidocytidine analogues against hepatitis C virus replication: the discovery of 4'-azidoarabinocytidine.
Smith DB, Kalayanov G, Sund C, Winqvist A, Pinho P, Maltseva T, Morisson V, Leveque V, Rajyaguru S, Le Pogam S, Najera I, Benkestock K, Zhou XX, Maag H, Cammack N, Martin JA, Swallow S, Johansson NG, Klumpp K, Smith M. Smith DB, et al. Among authors: klumpp k. J Med Chem. 2009 Jan 8;52(1):219-23. doi: 10.1021/jm800981y. J Med Chem. 2009. PMID: 19055482
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. Among authors: klumpp k. J Med Chem. 2009 May 14;52(9):2971-8. doi: 10.1021/jm801595c. J Med Chem. 2009. PMID: 19341305
129 results