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Identification of novel epoxide inhibitors of hepatitis C virus replication using a high-throughput screen |
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| Authors: | Peng Lee F Kim Sun Suk Matchacheep Sirinya Lei Xiaoguang Su Shun Lin Wenyu Runguphan Weerawat Choe Won-Hyeok Sakamoto Naoya Ikeda Masanori Kato Nobuyuki Beeler Aaron B Porco John A Schreiber Stuart L Chung Raymond T |
| Affiliation: | GI Unit, Department of Medicine, Massachusetts General Hospital, Boston, MA 02114, USA. |
| Abstract: | Using our high-throughput hepatitis C replicon assay to screen a library of over 8,000 novel diversity-oriented synthesis (DOS) compounds, we identified several novel compounds that regulate hepatitis C virus (HCV) replication, including two libraries of epoxides that inhibit HCV replication (best 50% effective concentration, < 0.5 microM). We then synthesized an analog of these compounds with optimized activity. |
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