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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 IVl--n were obtained by reaction of 3-(p-nitrophenyl)-4-phenyl-1H-pyrrole-2,5-dione potassium salt with the appropriate chloroalkylamine. Hydrogenation of IVl,n gave the the corresponding cis-3-(p-aminophenyl)-4-phenylsuccinimides (VIIIa,b). The structure-cytostatic activity relationship of these compounds is discussed.

Synthesis, structure and cytostatic activity of a series of N-substituted 3,4-diphenyl-1H-pyrrole-2,5-diones.