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 = 0.003 mu M), highly selective, and safe in in vitro and in vivo assays. (C) 2013 Elsevier Ltd. All rights reserved.
Discovery of an irreversible HCV NS5B polymerase inhibitor
Zeng, Q., Nair, A. G., Rosenblum, S. B., Huang, H-C., Lesburg, C. A., Jiang, Y., Selyutin, O., Chan, T-Y., Bennett, F., Chen, K. X., Venkatraman, S., Sannigrahi, M., Velazquez, F., Duca, J. S., Gavalas, S., Huang, Y., Pu, H., Wang, L., Pinto, P., ... Kozlowski, J. A. (2013). Discovery of an irreversible HCV NS5B polymerase inhibitor. Bioorganic and Medicinal Chemistry Letters, 23(24), 6585-6587. https://doi.org/10.1016/j.bmcl.2013.10.060
Abstract
Publications Info
To contact an RTI author, request a report, or for additional information about publications by our experts, send us your request.
Meet the Experts
View All ExpertsRecent Publications
Article
Multifaceted risk for non-suicidal self-injury only versus suicide attempt in a population-based cohort of adults
Article
Community overdose surveillance
Article
Epigenetic biomarkers for smoking cessation
Article