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.
一系列N-取代的
3,4-二苯基-1H-吡咯-2,5-二酮(二苯基马来
酰亚胺)(IV)被合成并测试了它们的细胞抑制活性。化合物IVa-k由二
苯基马来酸酐或其二硝基衍
生物(V或VI)与相应的胺制备。化合物IVI-n通过3-(对
硝基苯基)-4-苯基-1H-
吡咯-2,5-二酮
钾盐与适当
氯代烷基胺反应得到。IVI,n的氢化反应得到了相应的顺式-3-(对
氨基苯基)-4-苯基琥珀
酰亚胺(VIIIa,b)。这些化合物的结构-细胞抑制活性关系被讨论。