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Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity |
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| Authors: | Sheng X Christopher Casarez Anthony Cai Ruby Clarke Michael O Chen Xiaowu Cho Aesop Delaney William E Doerffler Edward Ji Mingzhe Mertzman Michael Pakdaman Rowchanak Pyun Hyung-Jung Rowe Tanisha Wu Qiaoyin Xu Jie Kim Choung U |
| Institution: | Gilead Sciences, Inc., 333 Lakeside Dr, Foster City, CA 94404, USA. csheng@gilead.com |
| 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. |
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