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. 2012 May 1;22(9):3265-8.
doi: 10.1016/j.bmcl.2012.03.021. Epub 2012 Mar 16.

Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication

Magnus Nilsson  1 , Genadiy Kalayanov, Anna Winqvist, Pedro Pinho, Christian Sund, Xiao-Xiong Zhou, Horst Wähling, Anna-Karin Belfrage, Michael Pelcman, Tatiana Agback, Kurt Benckestock, Kristina Wikström, Mirva Boothee, Anneli Lindqvist, Christina Rydegård, Tim H M Jonckers, Koen Vandyck, Pierre Raboisson, Tse-I Lin, Sophie Lachau-Durand, Herman de Kock, David B Smith, Joseph A Martin, Klaus Klumpp, Kenneth Simmen, Lotta Vrang, Ylva Terelius, Bertil Samuelsson, Sa Rosenquist, Nils Gunnar Johansson
Affiliations

Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication

Magnus Nilsson et al. Bioorg Med Chem Lett. .

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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