Synthesis and Evaluation of 2,6-Modified Purine 2′-<i>C</i>-Methyl Ribonucleosides as Inhibitors of HCV Replication

Longhu Zhou, Hongwang Zhang, Sijia Tao, Maryam Ehteshami, Jong Hyun Cho, Tamara R. McBrayer, Philip Tharnish, Tony Whitaker, Franck Amblard, Steven J. Coats,

ACS Medicinal Chemistry Letters · 2015 · 19 citations · 15 references

Concepts

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.

References

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