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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.
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
  • Nilsson M; Medivir AB, PO Box 1086, SE-141 22 Huddinge, Sweden. magnus.k.nilsson@telia.com
Bioorg Med Chem Lett ; 22(9): 3265-8, 2012 May 01.
Article in En | MEDLINE | ID: mdl-22472694
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Prodrugs / Hepacivirus / Cytidine / Deoxycytidine Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Antiviral Agents / Prodrugs / Hepacivirus / Cytidine / Deoxycytidine Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Document type: Article Affiliation country: