Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents
Discovery of novel 4(1H)-quinolone derivatives as potential antiproliferative and apoptosis inducing agents
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发现新型 4(1H)-喹诺酮衍生物作为潜在的抗增殖和细胞凋亡诱导剂
DOI：
10.1016/j.bmcl.2017.07.005
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发表时间：
2017-09-01
影响因子：
2.7
通讯作者：
Li, Fei
中科院分区：
文献类型：
--
作者：
Zhou, Ping;Huang, Linsheng;Li, Fei
合成了一系列新的4（1H）-喹诺酮衍生物，并进行了体外抗增殖活性的评价。结果表明，这些化合物对一组人肿瘤细胞系显示出比先导化合物7-氯-4（1H）-喹诺酮1更强的抗增殖作用。发现化合物7 e是最有效的抗增殖剂，并显示出对HepG 2细胞系的选择性细胞毒活性，IC 50值低于1.0 μ M。Annexin V/FITC-PI法显示化合物7 e诱导HepG 2细胞凋亡，并呈剂量依赖性。Western blotting分析表明，化合物7 e通过p53依赖性途径诱导细胞周期阻滞于G2/M期。(C)2017爱思唯尔有限公司版权所有
A series of novel 4(1H)-quinolone derivatives was synthesized and evaluated for antiproliferative activity in vitro. The results showed that these compounds exhibited more potent antiproliferative effect against a panel of human tumor cell lines than the lead compound 7-chloro-4(1H)-quinolone 1. Compound 7e was found to be the most potent antiproliferative agent and to exhibit selective cytotoxic activity against HepG2 cell lines with IC50 value lower than 1.0 mu M. Annexin V/FITC-PI assay showed that compound 7e induced apoptosis in HepG2 cells with a dose-dependent manner. Western blotting analysis indicated that compound 7e induced cell cycle arrest in G2/M phase by p53-depedent pathway. (C) 2017 Elsevier Ltd. All rights reserved.