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ID: ALA1955809

Journal: Bioorg Med Chem Lett

Title: Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity.

Authors: Sheng XC, Casarez A, Cai R, Clarke MO, Chen X, Cho A, Delaney WE, Doerffler E, Ji M, Mertzman M, Pakdaman R, Pyun HJ, Rowe T, Wu Q, Xu J, Kim CU.

Abstract: A potent and novel class of phosphinic acid derived product-like inhibitors of the HCV NS3/4A protease was discovered previously. Modification of the phosphinic acid and quinoline heterocycle led to GS-9256 with potent cell-based activity and favorable pharmacokinetic parameters. Based on these attributes, GS-9256 was advanced to human clinical trial as a treatment for chronic infection with genotype 1 HCV.

CiteXplore: 22244938

DOI: 10.1016/j.bmcl.2011.12.038