Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.
| Autor: | Nilsson M; Medivir AB, PO Box 1086, SE-141 22 Huddinge, Sweden. magnus.k.nilsson@telia.com, Kalayanov G, Winqvist A, Pinho P, Sund C, Zhou XX, Wähling H, Belfrage AK, Pelcman M, Agback T, Benckestock K, Wikström K, Boothee M, Lindqvist A, Rydegård C, Jonckers TH, Vandyck K, Raboisson P, Lin TI, Lachau-Durand S, de Kock H, Smith DB, Martin JA, Klumpp K, Simmen K, Vrang L, Terelius Y, Samuelsson B, Rosenquist S, Johansson NG |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3265-8. Date of Electronic Publication: 2012 Mar 16. |
| DOI: | 10.1016/j.bmcl.2012.03.021 |
| Abstrakt: | 4'-Azido-2'-deoxy-2'-methylcytidine (14) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC(50) value of 1.2 μM and showing moderate in vivo bioavailability in rat (F=14%). Here we describe the synthesis and biological evaluation of 4'-azido-2'-deoxy-2'-methylcytidine and prodrug derivatives thereof. (Copyright © 2012 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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