Design, synthesis and docking studies of novel 1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carboxamide derivatives as a potential anti-proliferative agents
Design, synthesis and docking studies of novel 1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carboxamide derivatives as a potential anti-proliferative agents
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DOI：
10.1016/j.ejmech.2016.09.062
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发表时间：
2017-01-05
影响因子：
6.7
通讯作者：
Manga, Vijjulatha
中科院分区：
文献类型：
--
作者：
Banu, Saleha;Bollu, Rajitha;Manga, Vijjulatha
使用肽偶联剂与取代的 N-苯基哌嗪和哌啶设计并合成了一系列新的 4-羟基-1-甲基-2-氧代-1,2-二氢喹啉-3-甲酰胺杂化物 8a-1，产率良好至优异。评估了合成化合物对 PANC 1、HeLa 和 MDA-MB-231 的体外抗增殖活性。化合物8d、8e、8f、8g、8h和8k表现出相当大的抗增殖活性，GI(50)值范围为0.15至1.4μM。活性化合物针对微管蛋白的计算机分子对接研究进一步支持了结构和抗增殖活性关系。 (C) 2016 Elsevier Masson SAS。版权所有。
A new series of 4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide hybrids 8a-1 have been designed and synthesized using peptide coupling agents with substituted N-phenyl piperazines and piperidines with good to excellent yields. The synthesized compounds were evaluated for their in vitro anti-proliferative activity against PANC 1, HeLa and MDA-MB-231. The compounds 8d, 8e, 8f, 8g, 8h and 8k exhibited considerable anti-proliferative activity with GI(50) values ranging from 0.15 to 1.4 mu M. The structure and anti-proliferative activity relationship was further supported by in silico molecular docking study of the active compounds against tubulin protein. (C) 2016 Elsevier Masson SAS. All rights reserved.