Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1,3,4-oxadiazole-2(3H)-thione quinolone derivatives as novel anticancer agent

被引：101

作者：

Sun, Juan ^{[1
]}

Zhu, Hui ^{[1
]}

Yang, Zhong-Ming ^{[1
]}

Zhu, Hai-Liang ^{[1
]}

机构：

[1] Shandong Univ Technol, Sch Life Sci, Zibo 255049, Shandong, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 60卷

关键词：

Quinoline; 1,3,4-Oxadiazole; Antiproliferative; Telomerase inhibitor; Molecular docking; ANTITUMOR; 1,4-BENZODIOXAN; DOCKING; DESIGN; MOIETY;

D O I：

10.1016/j.ejmech.2012.11.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of quinoline derivatives (4a-4o) have been synthesized and their biological activities were also evaluated as potential telomerase inhibitors. Bioassay tests demonstrated that most of the compounds exhibited substantial broad-spectrum antitumor activity against the three cancer cell lines (HepG2, SGC-7901 and MCF-7). Moreover, all the title compounds were assayed for telomerase inhibition using the TRAP-PCR-ELISA assay. Compounds 4d and 4i displayed the most potent anticancer activities, which were comparable to the positive control. Docking simulation was performed to position compounds 4d and 4i into the telomerase structure active site to determine the probable binding model. Compounds 4d and 4i with potent inhibitory activity in tumor growth inhibition may be potential anticancer agents. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：23 / 28

页数：6

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