Antitumor and DNA Topoisomerase II alpha Inhibitory Activity of 6-Substituted-aryl-2-methoxyquinolines

作者

Li, ZY;Ding, YJ;Bu, HG;Shen, YM

作者单位

[Li Zhiying; Bu Huagang; Shen Yuemao] Shandong Univ, Sch Pharmaceut Sci, Minist Educ, Key Lab Chem Biol, Jinan 250012, Shandong, Peoples R China.;-;[Ding Yanjiao] Shandong Univ, Shandong Prov Hosp, Dept Pharm, Jinan 250021, Shandong, Peoples R China.

摘要

Human DNA Topoisomerase II alpha (Topo II alpha) is one of the important therapeutic targets for the treatment of cancers. Our previous study showed that p-terphenyls have inhibitory effects on Topo II alpha and inhibit the proliferation of human breast ductal carcinoma cells. In this study, nineteen 6-substituted aryl-2-methoxyquinolines (3a similar to 3s) were designed, synthesized and evaluated for their cytotoxicity against the growth of human triple negative breast cancer MDA-MB-231 cell line and inhibitory activity against Topo II alpha. Among these compounds, 6-(4-(hydroxymethyl)phenyl)-2-methoxyquinoline (3b) showed the most potent activity (IC50 = 9.9 mu mol.L-1). These results have important significance for the further study of aryl quinoline TopoII alpha inhibitors.

关键词

基本信息

所属机构:

归属医师:

UT：000455093900007

刊名:CHINESE JOURNAL OF ORGANIC CHEMISTRY

年，卷(期):2018年38卷12期

页码：3204-3210

DOI：10.6023/cjoc201806015

附件：

收录: SCIE