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基于双吲哚马来酰亚胺化合物和硫脲化合物的结构及多样的生物活性,通过1-氨基-3,4-二(吲哚-3-基)-3-吡咯啉-2,5-二酮与异硫氰酸酯反应,合成了17种新的3,4-二(吲哚-3-基)-2,5-二酮-1-吡咯亚胺硫脲类化合物,化合物的结构通过1H NMR、13C NMR、HRMS等进行了表征。该系列化合物的初步抗肿瘤活性测试表明,它们都对细胞周期分裂蛋白25B(CDC 25B)表现出良好的抑制活性(大部分化合物的抑制率在96%以上),具有潜在的抗肿瘤活性及应用价值。
Based on the structures and diverse biological activities of bisindol maleimide compounds and thiourea compounds, the synthesis of 1-amino-3,4-bis (indol-3-yl) Seventeen novel 3,4-bis (indol-3-yl) -2,5-dione-1-pyrrolethiocarbazide compounds were synthesized by the reaction of diketones with isothiocyanates. The structures of the compounds Characterization by 1H NMR, 13C NMR, HRMS and so on. Preliminary antitumor activity tests of these compounds showed that all of them exhibited good inhibitory activity against cell cycle-associated protein 25B (CDC 25B) (96% inhibition rate for most compounds), potential antitumor activity and their application value.