Chinese Journal of Organic Chemistry >
Design, Synthesis and Anticancer Activity Studies of Novel Quinoline-Indole Derivatives
Received date: 2021-03-30
Revised date: 2021-05-25
Online published: 2021-06-29
Supported by
National Natural Science Foundation of China(81703541); National Natural Science Foundation of China(81673322); National Natural Science Foundation of China(U2004123); China Postdoctoral Science Foundation(2018M632812)
As the continuation of our studies on novel and effective anti-cancer agents, a series of novel quinoline-indole derivatives were firstly designed and synthesized by molecular hybridization strategy and Lewis acid‐catalyzed coupling reactions. Their antiproliferative potency on gastric cancer cell line MGC-803, colon cancer cell line HCT-116, and esophageal cancer cell line Kyse450 of all the targeted compounds was explored using methyl thiazolyl tetrazolium (MTT) assay. 2-Chloro-4-(5-methoxy-1H-indol-3-yl)quinoline (9b) exhibited potently inhibitory activity against MGC-803, HCT-116, and Kyse450 cells with IC50 values of 0.58, 0.68 and 0.59 µmol•L–1. Further mechanism studies suggested that compound 9b inhibited the cell colony formation of MGC-803 and HGC-27 cells. Compound 9b induced an intrinsic apoptosis and down- regulated the levels of apoptosis related proteins in MGC-803 and HGC-27 cells. Meanwhile, compound 9b arrested MGC-803 and HGC-27 cells at the G2/M phase. Taken together, these results indicated that compound 9b might be a valuable lead compound for anticancer agents.
Key words： quinoline; indole; anticancer activity; proliferation; apoptosis; cell cycle arrest
Shenghui Wang , Yongfeng Guan , Xiujuan Liu , Xinying Yuan , Guangxi Yu , Yinru Li , Yanbing Zhang , Jian Song , Wen Li , Saiyang Zhang . Design, Synthesis and Anticancer Activity Studies of Novel Quinoline-Indole Derivatives[J]. Chinese Journal of Organic Chemistry, 2021 , 41(9) : 3617 -3624 . DOI: 10.6023/cjoc202103059
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