Elsevier, Bioorganic and Medicinal Chemistry Letters, 24(23), p. 6585-6587
DOI: 10.1016/j.bmcl.2013.10.060
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The discovery of lead compound 2e was described. Its covalent binding to HCV NS5B polymerase enzyme was investigated by X-ray analysis. The results of distribution, metabolism and pharmacokinetics were reported. Compound 2e was demonstrated to be potent (replicon GT-1b EC50=0.003μM), highly selective, and safe in in vitro and in vivo assays.