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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 (author)
Kalayanov, Genadiy (author)
Winqvist, Anna (author)
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Pinho, Pedro (author)
Sund, Christian (author)
Zhou, Xiao- Xiong (author)
Wahling, Horst (author)
Belfrage, Anna Karin, 1977- (author)
Medivir AB, PO Box 1086, SE-141 22 Huddinge, Sweden
Pelcman, Michael (author)
Agback, Tatiana (author)
Benckestock, Kurt (author)
Wikström, Kristina (author)
Boothee, Mirva (author)
Lindqvist, Anneli (author)
Rydegard, Christina (author)
Jonckers, Tim H. M. (author)
Vandyck, Koen (author)
Raboisson, Pierre (author)
Lin, Tse-I (author)
Lachau-Durand, Sophie (author)
de Kock, Herman (author)
Smith, David B. (author)
Martin, Joseph A. (author)
Klumpp, Klaus (author)
Simmen, Kenneth (author)
Vrang, Lotta (author)
Terelius, Ylva (author)
Samuelsson, Bertil (author)
Rosenquist, Åsa (author)
Johansson, Nils Gunnar (author)
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 (creator_code:org_t)
Elsevier BV, 2012
2012
English.
In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 22:9, s. 3265-3268
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • 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.

Subject headings

NATURVETENSKAP  -- Kemi (hsv//swe)
NATURAL SCIENCES  -- Chemical Sciences (hsv//eng)

Keyword

hepatitis c virus
ns5b polymerase
antivirals
nucleoside
prodrug
phosphoramidate
genotype 1 infection
antiviral activity
viral-hepatitis
analogs
design
4'-azidocytidine
boceprevir
telaprevir
resistance

Publication and Content Type

ref (subject category)
art (subject category)

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