10-羟基喜树碱衍生物的合成及体外抑制肿瘤活性

Synthesis and antitumor activities of 10-hydroxy camptothecin derivatives

摘要: 目的寻找高效低毒的喜树碱类抗肿瘤新药。方法合成7个喜树碱衍生物（3~9），经¹HNMR，IR，MS分析确证了所合成化合物的结构，经MTT法筛选了对宫颈癌Hela、肝癌BEL-7402、胃癌7901和大肠癌CCL-187瘤株的体外抑制肿瘤活性。结果7个化合物分别对前三种瘤株有效，其中化合物4对前三种瘤株均有较好的体外抑制肿瘤细胞活性，尤其对宫颈癌Hela细胞的抑制活性大于10-羟基喜树碱。结论该类化合物的抗癌活性值得进一步研究。

Abstract: AimTo find new anticancer drug based on the structure of 10-hydroxy camptothecin. MethodsSeven camptothecin derivatives (3-9) were synthesized and the antitumor activities of these derivatives were evaluated. ResultsStructures of seven new compounds were determined by ¹HNMR, IR, MS. Seven compounds showed inhibitory effects on Hela, BEL-7402, 7901 cell lines in vitro. Especially, compound 4 showed high bioactivities to all of the tumor cells in vitro, its anticancer activity against human cervical carcinoma Hela was much higher than that of 10-hydroxy camptothecin. ConclusionSome compounds are worth further studying.