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

作者：Li, Zhiying; Ding, Yanjiao; Bu, Huagang; Shen, Yuemao^*

来源：Chinese Journal of Organic Chemistry, 2018, 38(12): 3204-3210.

DOI：10.6023/cjoc201806015

• Topoisomerase II alpha
• Synthesis
• Structure optimization
• Antitumor activity

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.

• 出版日期2018-12-25
• 单位山东省立医院; 山东大学