Synthesis, Structure and Cytostatic Activity of a Series of N-Substituted 3, 4-Diphenyl-1H-pyrrole-2, 5-diones

Abstract

A series of N-substituted 3, 4-diphenyl-1H-pyrrole-2, 5-diones (diphenylmaleimides)(IV) were synthesized and tested for cytostatic activity. Compounds IVa-k were prepared from diphenylmaleic anhydride or its dinitro derivative (V or VI) and the corresponding amine. Compounds IVI-n were obtained by reaction of 3-(p-nitrophenyl)-4-phenyl-1H-pyrrole-2, 5-dione potassium salt with the appropriate chloroalkylamine. Hydrogenation of IVI, n gave the the corresponding cis-3-(p-aminophenyl)-4-phenylsuccinimides (VIIIa, b). The structure-cytostatic activity relationship of these compounds is discussed.