SYNTHESIS OF SOME HALOGENATED INDIRUBIN DERIVATIVES

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 L₇₂₁₂ bearing mice and W₂₅₆ bearing rats than indirubin. In the parallel experiment, the most active compound Ⅲ showed increase in lifespan of mice bearing L₇₂₁₂ by 41～73%, and marked inhibitory action against W₂₅₆ in rats with the inhibition rates of 48～83%,while indirubin showed 0 and 30% inhibition.