2-芳基（烷基）-苯并咪唑-1-乙酰腙衍生物的合成及抗肿瘤活性研究

摘要

在2-取代苯并咪唑环上引入酰腙基团,合成了一系列含有苯并咪唑环的酰腙衍生物( c1-18),采用IR,1 H NMR和MS对其结构进行了表征,采用MTT法对目标物抑制4种癌细胞增殖活性进行了测试。其中N-(2,4-二羟基苯亚甲基)-2-[2-(2,4-二氯苯基)-1H-苯并咪唑-1-基]乙酰腙(c2)和N-(2-羟基苯甲烯基)-2-[2-(4-硝基苯基)-1H-苯并咪唑-1-基]乙酰腙(c10)对所测试的肿瘤细胞均表现出明显的抑制活性(IC50=2-21μM)。%A class of acetylhydrazone derivatives(c1-18)containing benzimidazole moieties were synthesized. Their structures were characterized by 1 H NMR, IR, and MS, and their antitumor activities against four cancer cells were determined by the MTT as-say. Among them N-(2,4-dihydroxybenzylidene)-2-(2-(2,4-dichlorophenyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide(c2)and N-(2-hydroxybenzylidene)-2-(2-(2,4-dichlorophenyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide(c10)displayed excellent canc-er inhibitory activity against the tested cancer cells( IC50=2-21 μM) compared with gefitinib.