Chin. J. Org. Chem. ›› 2009, Vol. 29 ›› Issue (05): 724-729. Previous Articles     Next Articles

Original Articles

20(S)-O-喜树碱肉桂酸酯衍生物的合成及其抗肿瘤活性研究

段华鑫a ; 张殊佳*,a,b ; 周 鹏a   

  1. (a大连大学环境与化学工程学院 大连 116622)
    (b辽宁省生物有机化学重点实验室 大连 116622)
  • 收稿日期:2008-08-03 修回日期:2008-10-29 发布日期:2009-05-20
  • 通讯作者: 张殊佳

Synthesis and Antitumor Activity of 20(S)-O-Linked Camptothecin Cinnamic Acid Ester Derivatives

Duan, Huaxina ; Zhang, Shujia*,a,b ; Zhou, Penga   

  1. (a College of Environmental and Chemical Engineering, Dalian University, Dalian 116622)
    (b Key Laboratory of Bioorganic Chemistry of Liaoning Province, Dalian 116622)
  • Received:2008-08-03 Revised:2008-10-29 Published:2009-05-20
  • Contact: Zhang, Shujia

In order to increase the stability of lactone ring of camptothecin and decrease its toxicity or increase its potency of antitummors, the camptothecin structure was modified and 17 camptothecin cinnamic acid ester derivatives were synthesized by straightforward esterification of camptothecin with the corresponding acid. And their antitumor activities in vitro were evaluated against human cancer cell SGC-7901 by a MTT method. The preliminary experimental results showed that the bioactivities of some derivatives of campto-thecin were higher than that of their parent against SGC-7901.

Key words: cinnamic acid, synthesis, antitumor activi, camptothecin derivative