Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (6): 1598-1607.DOI: 10.6023/cjoc201911028 Previous Articles     Next Articles

新型香豆素类衍生物的合成及抗肿瘤活性研究

时蕾a, 李子秋a, 崔鑫鑫b, 朱挺b, 庞晓静b, 李龙辉a, 罗德福a, 刘方芳b, 赵冰玉b, 龙跃a, 张赛扬c   

  1. a 郑州大学化学学院 郑州 450001;
    b 郑州大学药学院 郑州 450001;
    c 郑州大学基础医学院 郑州 450001
  • 收稿日期:2019-11-23 修回日期:2020-01-15 发布日期:2020-04-09
  • 通讯作者: 龙跃, 张赛扬 E-mail:longyue@zzu.edu.cn;saiyangz@zzu.edu.cn
  • 基金资助:
    国家自然科学基金(Nos.81703541,81673322)和中国博士后科学基金(No.2018M632812)资助项目.

Synthesis and Anticancer Activity of Novel Coumarin Derivatives

Shi Leia, Li Ziqiua, Cui Xinxinb, Zhu Tingb, Pang Xiaojingb, Li Longhuia, Luo Defua, Liu Fangfangb, Zhao Bingyub, Long Yuea, Zhang Saiyangc   

  1. a College of Chemistry, Zhengzhou University, Zhengzhou 450001;
    b School of Pharmaceutical Sciences, Zhengzhou 450001;
    c School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001
  • Received:2019-11-23 Revised:2020-01-15 Published:2020-04-09
  • Supported by:
    Project supported by the National Natural Sciences Foundations of China (Nos. 81703541, 81673322) and the China Postdoctoral Science Foundation (No. 2018M632812).

Nineteen novel 3,4,5-trimethoxyphenyl 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-trimethoxy-phenyl)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 μmol/L.

Key words: coumarin, anticancer, synthesis