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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

  作者 Sheng, XC; Casarez, A; Cai, R; Clarke, MO; Chen, XW; Cho, A; Delaney, WE; Doerffler, E; Ji, MZ; Mertzman, M; Pakdaman, R; Pyun, HJ; Rowe, T; Wu, QY; Xu, J; Kim, CU  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-3;  页码  1394-1396  
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[摘要]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. (C) 2011 Published by Elsevier Ltd.

 
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