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Research article2012Peer reviewed

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

Nilsson, Magnus; Kalayanov, Genadiy; Winqvist, Anna; Pinho, Pedro; Sund, Christian; Zhou, Xiao-Xiong; Wahling, Horst; Belfrage, Anna-Karin; Pelcman, Michael; Agback, Tatiana; Benckestock, Kurt; Wikstrom, Kristina; Boothee, Mirva; Lindqvist, Anneli; Rydegard, Christina; Jonckers, Tim H. M.; Vandyck, Koen; Raboisson, Pierre; Lin, Tse-I; Lachau-Durand, Sophie;
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Abstract

4'-Azido-2'-deoxy-2'-methylcytidine (14) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC50 value of 1.2 mu M 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. (C) 2012 Elsevier Ltd. All rights reserved.

Keywords

Hepatitis C virus; NS5B polymerase; Antivirals; Nucleoside; Prodrug; Phosphoramidate

Published in

Bioorganic and Medicinal Chemistry Letters
2012, Volume: 22, number: 9, pages: 3265-3268 Publisher: PERGAMON-ELSEVIER SCIENCE LTD

      UKÄ Subject classification

      Medicinal Chemistry
      Pharmacology and Toxicology

      Publication identifier

      DOI: https://doi.org/10.1016/j.bmcl.2012.03.021

      Permanent link to this page (URI)

      https://res.slu.se/id/publ/99459