Synthesis, structure and cytostatic activity of a series of N-substituted 3,4-diphenyl-1H-pyrrole-2,5-diones.
作者:Miguel Fernandez BRANA、Ascension FERNANDEZ、Mercedes GARRIDO、Maria Luz Lopez RODRIGUEZ、M. Jose MORCILLO、Antonio M. SANZ
DOI:10.1248/cpb.37.2710
日期:——
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。