若干卤代靛玉红衍生物的合成  

SYNTHESIS OF SOME HALOGENATED INDIRUBIN DERIVATIVES

作　　者：顾月翠[1] 李国林[1] 杨尧平[1] 付建平[1] 李成章[1] 

机构地区：[1]四川省中药研究所,重庆630065

出　　处：《药学学报》1989年第8期629-632,共4页Acta Pharmaceutica Sinica

摘　　要：靛玉红用于临床治疗慢性粒细胞白血病已有多年,疗效明确。但溶解度差,影响在体内的吸收。近年来为了提高疗效降低肠胃道副作用,在亚氨基和羰基上合成了一系列化合物,并筛选出一些有抗肿瘤作用的活性物质,在靛玉红芳环上的卤代物,虽有Eller-Pandrand等作过一些工作,但未见用于抗肿瘤上,本文在芳环上引进卤素拟增加溶解度,共合成了6个卤代靛玉红,经药理抗肿瘤筛选,在平行试验中,化合物Ⅰ,Ⅱ。Indirubin has been used clinically to treat chronic granulocytic leukemia, but poor solubility limited its absorption in the body. In order to reduce its side effect and raise its therapeutic effect on chronic granulocytic leukemia, six halogen-substituted derivatives were synthesized. Compounds Ⅰ,Ⅱ,Ⅲ and Ⅴ exhibited higher antitumor activity against L_(7212) bearing mice and W_(256) bearing rats than indirubin. In the parallel experiment, the most active compound Ⅲ showed increase in lifespan of mice bearing L_(7212) by 41～73%, and marked inhibitory action against W_(256) in rats with the inhibition rates of 48～83%,while indirubin showed 0 and 30% inhibition.

关 键 词：卤代靛玉红 吲哚酚 卤代吲哚醌 

分 类 号：R914.5[医药卫生—药物化学]