SIOC English
有机化学
高级检索

有机化学 ›› 2009, Vol. 29 ›› Issue (05): 724-729. 上一篇    下一篇

研究论文

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

PDF

1199

被引次数

13

为了提高喜树碱内酯环的稳定性降低其毒性, 增加其抗肿瘤效能, 以喜树碱为先导化合物, 通过酯化反应直接合成了17个20(S)-喜树碱肉桂酸酯衍生物, 并采用MTT法测定了对于人胃癌细胞SGC-7901的体外抗肿瘤活性, 活性测试结果表明有些化合物的抑制活性明显高于母体化合物喜树碱.

关键词: 肉桂酸, 合成, 抗肿瘤活性
, 喜树碱衍生物

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