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取代肉桂酸苯乙酯的抗肿瘤活性研究

李树春, 李辉, 张法, 李中军*, 崔景荣**   

  1. 1.北京大学药学院化学生物学系;
    2.北京大学天然药物及仿生药物国家重点实验室, 北京 100083
  • 收稿日期:2003-07-15 修回日期:2003-11-10 出版日期:2003-12-15 发布日期:2003-12-15
  • 通讯作者: 李中军*, 崔景荣**

Anticancer Activities of Substituted Cinnamic Acid Phenethyl Esters on Human Cancer Cell Lines

LI Shu-chun, LI Hui, ZHANG Fa, LI Zhong-jun*, CUI Jing-rong**   

  1. 1.Department of Chemical Biology, School of Pharmaceutical Sciences;
    2.State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China
  • Received:2003-07-15 Revised:2003-11-10 Online:2003-12-15 Published:2003-12-15
  • Contact: LI Zhong-jun*, CUI Jing-rong**

摘要: 设计、合成了咖啡酸苯乙酯及16个取代肉桂酸苯乙酯化合物,并用MTT法或SRB法对其抗肿瘤活性进行了体外筛选。结果显示咖啡酸苯乙酯对HL-60Bel-7402Hela细胞有较好的抑制活性; 3,4-二甲氧基肉桂酸苯乙酯对Hela细胞有非常好的抑制活性; 4-丙酮氧基肉桂酸苯乙酯对Bel-7402细胞有非常好的抑制活性。

关键词: 药物化学, 取代肉桂酸苯乙酯, 合成, 抗肿瘤活性

Abstract: Caffeic acid phenethyl ester (CAPE) and sixteen substituted cinnamic acid phenethyl esters were prepared via conventional procedures in order to test their in vitro anticancer activities by either MTT assay or SRB assay on six different human cancer cell lines. The results indicated that in the concentration of 10 μmol·L-1 the lead compound CAPE possessed anticancer activities against human HL-60, Bel-7402, and Hela cell lines, and two other compounds possessed potent anticancer activities against Bel-7402 and Hela cell lines.

Key words: medicinal chemistry, medicinal chemistry, cinnamic acid phenethyl esters, cinnamic acid phenethyl esters, chemical synthesis, chemical synthesis, anticancer activity, anticancer activity

中图分类号: 

Supporting: Foundation item: National Science Foundation of China (30070887).
*Corresponding author. Tel.: 010-82801504; fax: 010-62367134;
**Tel.: 010-82802467