2. Academic Validation
  3. Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors

Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors

  • Bioorg Med Chem Lett. 2015 Mar 1;25(5):1040-3. doi: 10.1016/j.bmcl.2015.01.021.
Thorsten A Kirschberg 1,  Michael R Mish 1,  Lijun Zhang 1,  Neil H Squires 1,  Ke-Yu Wang 1,  Aesop Cho 1,  Joy Y Feng 1,  Martijn Fenaux 1,  Darius Babusis 1,  Yeojin Park 1,  Adrian S Ray 1,  Choung U Kim 1
Affiliations

Affiliation

  • 1 Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94044, USA.
PMID: 25650256 DOI: 10.1016/j.bmcl.2015.01.021
Abstract

The first synthesis of 1'-C-CN, 2'-F, 2'-C-Me pyrimidines is described. Anti-HCV activity was assessed and compared to the 1'-C-CN, 2'-C-Me as well as the 2'-F, 2'-C-Me pyrimidines. A phosphoramidate prodrug of the cytidine derivative showed activity in the low micromolar range against HCV replicons.

Keywords

HCV antivirals; Nucleotide phosphoramidate prodrugs; Pyrimidine nucleoside analogs.

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