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  

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

作　　者：段华鑫[1] 张殊佳[1,2] 周鹏[1] 

机构地区：[1]大连大学环境与化学工程学院,大连116622 [2]辽宁省生物有机化学重点实验室,大连116622

出　　处：《有机化学》2009年第5期725-730,共6页Chinese Journal of Organic Chemistry

摘　　要：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.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 camptothecin were higher than that of their parent against SGC-7901.

关 键 词：喜树碱衍生物 肉桂酸 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R730.5[医药卫生—药学]