Synthesis and Antitumor Activity of Indolemalylimide Derivatives

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 similar to 5t were synthesized. Starting with 5-nitroindole and different N-(3-chloropropyl)tertiary amines, followed by substitution, reduction and condensation, diindolyl derivatives 9a similar to 9f were synthesized. Twenty six novel compounds were synthesized, and their structures were confirmed by ESI-MS, elemental analysis and H-1 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.