苯并咪唑衍生物的合成及抗癌活性  

Synthesis and anticancer activity of benzimidazole derivatives

作　　者：胡莎莎 卿宾阳 王坚毅[1,3] HU Sha-sha;QING Bin-yang;WANG Jian-yi(College of Chemistry and Chemical Engineering,Guangxi University,Nanning 530004,China;College of Life Science and Technology,Guangxi University,Nanning 530004,China;Medical College,Guangxi University,Nanning 530004,China)

机构地区：[1]广西大学化学化工学院,广西南宁530004 [2]广西大学生命与科学技术学院,广西南宁530004 [3]广西大学医学院,广西南宁530004

出　　处：《化学研究与应用》2023年第1期145-150,共6页Chemical Research and Application

基　　金：国家自然科学基金项目(21967003)资助。

摘　　要：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.

关 键 词：抗癌 苯并咪唑 PARP 合成 

分 类 号：O622.6[理学—有机化学]