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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

  作者 Nilsson, M; Kalayanov, G; Winqvist, A; Pinho, P; Sund, C; Zhou, XX; Wahling, H; Belfrage, AK; Pelcman, M; Agback, T; Benckestock, K; Wikstrom, K; Boothee, M; Lindqvist, A; Rydegard, C; Jonckers, THM; Vandyck, K; Raboisson, P; Lin, TI; Lachau-Durand, S; de Kock, H; Smith, DB; Martin, JA; Klumpp, K; Simmen, K; Vrang, L; Terelius, Y; Samuelsson, B; Rosenquist, A; Johansson, NG  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-9;  页码  3265-3268  
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[摘要]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.

 
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