Synthesis and biological evaluation of novel anti-hepatitis C virus (HCV) agents: 2-hydroxylphenethyl sulfanyl-oxopyrimidines

被引：0
作者：
Daochun Wu
Yue Feng
Hua Wang
Junfeng Yang
Xian Chen
Yueping Wang
Christopher Cong Lai
Yufang Zhang
Cong Li
Xueshan Xia
Yanping He
机构：
[1] Yunnan University,Key Laboratory of Medicinal Chemistry for Natural Resources, Ministry of Education, School of Chemical Science and Technology
[2] Kunming University of Science and Technology,College of Life Science and Technology
[3] National Cancer Institute,Chemical Biology Laboratory, Center for Cancer Research
来源：
Medicinal Chemistry Research | 2017年 / 26卷
关键词：
Anti-HCV activity; Drug Discovery; Pyrimidone; HCV NS5B; SAR;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A novel series of dihydro-hydroxyl-phene-thylsulfanyl-ω-cyclohexyl/phenyl-oxopyrimidine derivatives have been synthesized and their in vitro anti-hepatitis C virus activities have been evaluated using Huh 7.5.1 cells. Some of the compounds showed moderate anti-hepatitis C virus activities, with EC50 range from 7.53 to 0.13 μM. Among all the compounds, 6-(cyclohexylmethyl)-5-ethyl-2-((2-hydroxy-2-phenylethyl)thio)-pyrimidin-4 (3H)-one (3a) had the most promising potential in inhibiting hepatitis C virus with an EC50 value of 0.13 μM and SI value of 121. It was noticed that some of these compounds are both active on hepatitis C virus and human immunodeficiency virus. In addition to experimental evaluation, structure-activity relationships and the molecular modeling analysis of these new congeners are also discussed.
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页码：1388 / 1396
页数：8
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