To discover novel compounds with antitumor activities, a series of indolylmaleimide derivatives were designed, synthesized and evaluated for their antitumor activities in vitro. Starting with indole and 2-chloroacetamide, followed by substitution and condensation, monoindolyl derivatives 5a～5t were syn-thesized. Starting with 5-nitroindole and different N-(3-chloropropyl)tertiary amines, followed by substitu-tion, reduction and condensation, diindolyl derivatives 9a～9f were synthesized. Twenty six novel com-pounds were synthesized, and their structures were confirmed by ESI-MS, elemental analysis and 1H NMR. The antitumor activities of the target compounds were evaluated with HL60, ECA-109, A549, SMMC-7721 and PC-3 in vitro. The in vitro antitumor activity showed that some compounds displayed inhibition to a certain degree against tested cells.

Key words: synthesis, antitumor, indolylmaleimide derivative