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Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication |
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| Authors: | Nilsson Magnus Kalayanov Genadiy Winqvist Anna Pinho Pedro Sund Christian Zhou Xiao-Xiong Wähling Horst Belfrage Anna-Karin Pelcman Michael Agback Tatiana Benckestock Kurt Wikström Kristina Boothee Mirva Lindqvist Anneli Rydegård Christina Jonckers Tim H M Vandyck Koen Raboisson Pierre Lin Tse-I Lachau-Durand Sophie de Kock Herman Smith David B Martin Joseph A Klumpp Klaus Simmen Kenneth Vrang Lotta Terelius Ylva Samuelsson Bertil Rosenquist Sa Johansson Nils Gunnar |
| Affiliation: | Medivir AB, PO Box 1086, SE-141 22 Huddinge, Sweden. magnus.k.nilsson@telia.com |
| Abstract: | 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. |
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