新型吲哚咔唑化合物的合成与抗肿瘤活性

Synthesis and Bioactivities of Novel Indolocarbazole Derivatives

设计合成了一系列吲哚咔唑结构的抗肿瘤新化合物.通过对反应溶剂进行选择和调整,优化了吲哚咔唑母核合成的反应条件,使后处理更为简便.用溴化噻唑蓝四氮唑(MTT)法对所合成的9个目标化合物进行了体外细胞毒活性测试,结果表明,化合物4a,4b,4d,4f和4i对人结肠癌HCT116和鼠白血病P388细胞的活性均强于阳性对照ED-571,其中化合物4f对P388细胞的活性是阳性对照的10倍.

A series of novel indoloearbazole derivatives was designed and synthesized. The solvent was studied and the reaction conditions including solvent choice were optimized via easier operations, The cytotoxicities of the 9 target compounds were tested using MTT methods. The results indicate that compounds 4a, 4b, 4d, 4f and 4i show better in vitro activities against HCT116 and P388 than positive control ED-571 did. Particularly, compound 4f is 10 times more potential against P388 than ED-571.