Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity
Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity
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DOI：
10.1016/j.bmcl.2012.04.096
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发表时间：
2012-06-15
影响因子：
2.7
通讯作者：
Cotelle, Philippe
中科院分区：
文献类型：
--
作者：
Suchaud, Virginie;Bailly, Fabrice;Cotelle, Philippe
本文报道了一系列3-羟基喹啉-2(1H)-酮衍生物的合成。在基础支架的第4位引入了酯和酰胺基团，并对苯基进行了一些调节。大多数化合物对HIV-1逆转录酶相关核糖核酸酶H的活性在10-20 mU M范围内表现出选择性抑制，而不影响整合酶和逆转录酶DNA聚合酶的活性。不幸的是，所有被测试的化合物在细胞培养中都表现出高度的细胞毒性，这限制了它们作为抗病毒药物的应用。(C)2012爱思唯尔有限公司。保留所有权利。
We report herein the synthesis of a series of 3-hydroxyquinolin-2(1H)-one derivatives. Esters and amide groups were introduced at position 4 of the basis scaffold and some modulations of the benzenic moiety were performed. Most compounds presented selective inhibitory properties in the 10-20 mu M range against HIV-1 reverse transcriptase associated ribonuclease H activity, without affecting the integrase and reverse transcriptase DNA polymerase activities. Unfortunately all tested compounds exhibited high cellular cytotoxicity in cell culture which limited their applications as antiviral agents. (C) 2012 Elsevier Ltd. All rights reserved.