Design, Synthesis and Anticancer Activity Studies of Novel Trimethoxyphenyl-quinoline Derivatives

被引：6
|
作者：
Wu, Bowen [1 ,3 ]
Cui, Xinxin [1 ,3 ]
Zhu, Ting [1 ,3 ]
Wang, Shenghui [2 ]
Lu, Chaofan [2 ]
Wang, Jinjie [1 ,3 ]
Dang, Hexiang [1 ,3 ]
Zhang, Saiyang [1 ,2 ,4 ]
Ding, Li'na [1 ,3 ]
Jin, Chengyun [1 ,3 ]
机构：
[1] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Henan, Peoples R China
[2] Zhengzhou Univ, Sch Basic Med Sci, Zhengzhou 450001, Peoples R China
[3] Minist Educ, Key Lab Adv Drug Preparat Technol, Zhengzhou 450001, Peoples R China
[4] Zhengzhou Univ, Henan Inst Adv Technol, Zhengzhou 450001, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 04期
基金：
中国博士后科学基金; 中国国家自然科学基金;
关键词：
quineline; trimethoxyphenyl; anticancer; cell cycle arrest; apoptosis; CELL LUNG-CANCER; BIOLOGICAL EVALUATION; ANTITUMOR; INHIBITORS; DOCKING; HYBRIDS;
D O I：
10.6023/cjoc201909016
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
With the expectation to find out novel and effective anti-tumor agents, a series of novel trimethoxyphenyl-quinoline 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 mu mol/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.
引用
收藏
页码：978 / 987
页数：10
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