Design, Synthesis and Anticancer Activity Studies of Novel Trimethoxyphenyl-quinoline Derivatives
Design, Synthesis and Anticancer Activity Studies of Novel Trimethoxyphenyl-quinoline Derivatives
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新型三甲氧基苯基喹啉衍生物的设计、合成及抗癌活性研究
DOI：
10.6023/cjoc201909016
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发表时间：
2020-04-25
影响因子：
1.9
通讯作者：
Jin, Chengyun
中科院分区：
文献类型：
--
作者：
Wu, Bowen;Cui, Xinxin;Jin, Chengyun
With the expectation to find out novel and effective anti-tumor agents, a series of novel trimethoxyphenylquinoline hybrids were designed, synthesized and evaluated for antiproliferative activity against three human cancer cell lines (EC-109, human esophageal cancer cells; PC-3, human prostate cancer cells; MGC-803, human gastric cancer cells). N-(3(Chloromethyl)benzyl)-3,4,5-trimethoxy-N-(quinolin-8-yl)benzamide (12j) showed the most potent antitumor activity against PC-3 cells with IC50 value of 9.23 μmol/L. Meanwhile, compound 12j inhibited the cell viability and colony formation of PC-3 cells. Further mechanism studies revealed that compound 12j could arrest PC-3 cells in G2/M phase and induce cell apoptosis via activating intrinsic and extrinsic apoptosis pathway.
