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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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2012 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1464-3405, Vol. 22, no 9, 3265-3268 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2012. Vol. 22, no 9, 3265-3268 p.
Keyword [en]
hepatitis c virus, ns5b polymerase, antivirals, nucleoside, prodrug, phosphoramidate, genotype 1 infection, antiviral activity, viral-hepatitis, analogs, design, 4'-azidocytidine, boceprevir, telaprevir, resistance
National Category
Chemical Sciences
URN: urn:nbn:se:uu:diva-212500DOI: 10.1016/j.bmcl.2012.03.021ISI: 000302964300045OAI: oai:DiVA.org:uu-212500DiVA: diva2:678094

928EN Times Cited:1 Cited References Count:21

Available from: 2013-12-11 Created: 2013-12-11 Last updated: 2013-12-11Bibliographically approved

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Belfrage, Anna Karin
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