Literature DB >> 22244938

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

X Christopher Sheng1, Anthony Casarez, Ruby Cai, Michael O Clarke, Xiaowu Chen, Aesop Cho, William E Delaney, Edward Doerffler, Mingzhe Ji, Michael Mertzman, Rowchanak Pakdaman, Hyung-Jung Pyun, Tanisha Rowe, Qiaoyin Wu, Jie Xu, Choung U Kim.   

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.
Copyright © 2011. Published by Elsevier Ltd.

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Year:  2011        PMID: 22244938     DOI: 10.1016/j.bmcl.2011.12.038

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Hepatitis C virus molecular evolution: transmission, disease progression and antiviral therapy.

Authors:  Maria Victoria Preciado; Pamela Valva; Alejandro Escobar-Gutierrez; Paula Rahal; Karina Ruiz-Tovar; Lilian Yamasaki; Carlos Vazquez-Chacon; Armando Martinez-Guarneros; Juan Carlos Carpio-Pedroza; Salvador Fonseca-Coronado; Mayra Cruz-Rivera
Journal:  World J Gastroenterol       Date:  2014-11-21       Impact factor: 5.742

2.  Illustrating and homology modeling the proteins of the Zika virus.

Authors:  Sean Ekins; John Liebler; Bruno J Neves; Warren G Lewis; Megan Coffee; Rachelle Bienstock; Christopher Southan; Carolina H Andrade
Journal:  F1000Res       Date:  2016-03-03

Review 3.  Current therapy for chronic hepatitis C: The role of direct-acting antivirals.

Authors:  Guangdi Li; Erik De Clercq
Journal:  Antiviral Res       Date:  2017-02-24       Impact factor: 5.970

4.  A nanoluciferase SARS-CoV-2 for rapid neutralization testing and screening of anti-infective drugs for COVID-19.

Authors:  Xuping Xie; Antonio E Muruato; Xianwen Zhang; Kumari G Lokugamage; Camila R Fontes-Garfias; Jing Zou; Jianying Liu; Ping Ren; Mini Balakrishnan; Tomas Cihlar; Chien-Te K Tseng; Shinji Makino; Vineet D Menachery; John P Bilello; Pei-Yong Shi
Journal:  Nat Commun       Date:  2020-10-15       Impact factor: 14.919

5.  Characterization of Hepatitis C virus resistance from a multiple-dose clinical trial of the novel NS5A inhibitor GS-5885.

Authors:  Kelly A Wong; Angela Worth; Ross Martin; Evguenia Svarovskaia; Diana M Brainard; Eric Lawitz; Michael D Miller; Hongmei Mo
Journal:  Antimicrob Agents Chemother       Date:  2013-07-22       Impact factor: 5.191

  5 in total

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