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

作　　者：李庆勇[1] 祖元刚[1] 付玉杰[1] 张莹[1] 刘群[2] 

机构地区：[1]东北林业大学森林植物生态学教育部重点实验室,黑龙江哈尔滨150040 [2]东北师范大学化学学院,吉林长春130024

出　　处：《药学学报》2004年第7期521-524,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目 ( 3 0 0 70 610 )

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 (39) ,经1 HNMR ,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 74 0 2、胃癌 790 1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。Aim To find new anticancer drug based on the structure of 10-hydroxy camptothecin. Methods Seven camptothecin derivatives (3-9) were synthesized and the antitumor activities of these derivatives were evaluated. Results Structures 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. Conclusion Some compounds are worth further studying.

关 键 词：10-羟基喜树碱 衍生物 抗癌活性 

分 类 号：R916.41[医药卫生—药学] R916.696