Synthesis and Anticancer Activity of Novel Coumarin Derivatives

被引:4
作者
Shi, Lei [1 ]
Li, Ziqiu [1 ]
Cui, Xinxin [2 ]
Zhu, Ting [2 ]
Pang, Xiaojing [2 ]
Li, Longhui [1 ]
Luo, Defu [1 ]
Liu, Fangfang [2 ]
Zhao, Bingyu [2 ]
Long, Yue [1 ]
Zhang, Saiyang [3 ]
机构
[1] Zhengzhou Univ, Coll Chem, Zhengzhou 450001, Peoples R China
[2] Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China
[3] Zhengzhou Univ, Sch Basic Med Sci, Zhengzhou 450001, Peoples R China
基金
中国博士后科学基金;
关键词
coumarin; anticancer; synthesis; AMIDE;
D O I
10.6023/cjoc201911028
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Nineteen novel 3,4,5-trimethoxyphenvl coumarin derivatives have been synthesized and evaluated for antitumor activity against three human cancer cell lines (EC-109, PC-3 and MGC-803). These chemical structures were well characterized by NMR and HRMS spectroscopic methods. N-Benzyl-2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)-N-(3,4,5-trimethoxyphenyl)acetamide) (4a) and N-((5-chlorobenzo[b]thiophen-3-yl)methyl)-2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy-N-(3,4,5-trimethoxyphenyl)acetamide) (4n) had better inhibitory activity against three kinds of tumor cells than 5-fluorouracil. Compound 4n showed the most potent antitumor activity against PC-3 cells with an IC50 value of 4.18 mu mol/L.
引用
收藏
页码:1598 / 1607
页数:10
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