Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro
Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro
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DOI：
10.1016/j.bmc.2010.06.058
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发表时间：
2010-08-15
影响因子：
3.5
通讯作者：
Ciliberto, Gennaro
中科院分区：
文献类型：
--
作者：
Sellitto, Grazia;Faruolo, Aurora;Ciliberto, Gennaro
制备了一系列1H-吲哚-3-羧酸乙酯9a（1-6）和9 b（1-2），并在Huh-7.5细胞中进行了评价。大部分化合物在低浓度下具有抗丙型肝炎病毒（HCV）活性。化合物9a（2）（> 10; > 16.7）和9 b（1）（> 6.25; > 16.7）的进入和复制抑制选择性指数高于其它评价化合物，包括先导化合物阿比朵尔（ARB，6; 15）。化合物9a（3）的选择性抑制指数大于ARB（6）（> 6.25）。在这三种初始命中中，化合物9a（2）是最有效的。(C)2010爱思唯尔有限公司保留所有权利。
A series of ethyl 1H-indole-3-carboxylates 9a(1-6) and 9b(1-2) were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity indices of inhibition on entry and replication of compounds 9a(2) (> 10; > 16.7) and 9b(1) (> 6.25; > 16.7) were higher than those of the other evaluated compounds, including the lead compound Arbidol (ARB, 6; 15). Moreover, the selective index of inhibition on entry of compound 9a(3) (> 6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a(2) was the most potent. (C) 2010 Elsevier Ltd. All rights reserved.