1. Academic Validation
  2. Synthesis and Evaluation of 2,6-Modified Purine 2'-C-Methyl Ribonucleosides as Inhibitors of HCV Replication

Synthesis and Evaluation of 2,6-Modified Purine 2'-C-Methyl Ribonucleosides as Inhibitors of HCV Replication

  • ACS Med Chem Lett. 2015 Nov 23;7(1):17-22. doi: 10.1021/acsmedchemlett.5b00402.
Longhu Zhou 1 Hongwang Zhang 1 Sijia Tao 1 Maryam Ehteshami 1 Jong Hyun Cho 1 Tamara R McBrayer 2 Philip Tharnish 2 Tony Whitaker 2 Franck Amblard 1 Steven J Coats 2 Raymond F Schinazi 1
Affiliations

Affiliations

  • 1 Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center , Atlanta, Georgia 30322, United States.
  • 2 CoCrystal Pharma, Inc. , Tucker, Georgia 30084, United States.
Abstract

A variety of 2,6-modified purine 2'-C-methylribonucleosides and their phosphoramidate prodrugs were synthesized and evaluated for inhibition of HCV RNA replication in Huh-7 cells and for cytotoxicity in various cell lines. Cellular pharmacology and HCV polymerase incorporation studies on the most potent and selective compound are reported.

Keywords

HCV; antiviral; nucleoside; phosphoramidate prodrug; purine.

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