IC50 值为 31 nmol/L, 并能显著抑制异柠檬酸脱氢酶 1 突变(R132H)型人脑星形胶质母细胞瘤细胞中 2-HG 的产生. 根据 实验数据进行了初步的构效关系讨论和分子模拟研究. 关键词 3-(吲哚-3-基)-4-(吡唑并[3,4-c]哒嗪-3-基)马来酰亚胺; 异柠檬酸脱氢酶 1 突变体(R132H)抑制剂; 合成; 生物 活性 Synthesis and Evaluation of 3-(Indol-3-yl)-4-(pyrazolo[3,4c]pyridazin-3-yl)maleimides as Potent Mutant Isocitrate Dehydrogenase-1 Inhibitors

3-Chloro-4-indolylmaleimides and two different alkynes are used as the starting materials in a novel and highly effective Pd-catalyzed addition/C–H activation/cyclization sequence for the synthesis of pyrrolo[3,4- c]carbazole-1,3(2 H,6 H)-diones. The desired products are obtained in moderate to excellent yields. Such compounds show a wide range of biological activities.