苯并咪唑衍生物的合成及抗癌活性

Synthesis and anticancer activity of benzimidazole derivatives

为了获得具有抗癌活性的新型PARP抑制剂,以2-氨基-3-硝基苯甲酸为原料,通过酯化、硝基还原等反应合成了8个苯并咪唑衍生物。合成的中间体及目标化合物结构经过了核磁共振氢谱、碳谱、质谱的确证。计算机类药性评价和MTT实验表明,目标化合物具有良好的类药性质,其中化合物HSS04表现出了与阳性药相当的抗增殖活性。

In order to obtain novel PARP inhibitors with anticancer activity,8 benzimidazole derivatives were synthesized by esterification and nitro reduction using 2-amino-3-nitrobenzoic acid as primary reactant.The structures of the synthesized intermediates and target compounds had been confirmed by 1H NMR,13 C NMR and HRMS.Drug-like property evaluation and MTT experiments showed that the target compounds had good drug-like properties.Especially the compound HSS04 exhibited antiproliferative activity equivalent to the positive drug.