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  

Synthesis and antitumor activity evaluation of 2-(2-aryl(alkyl)-1H-benzo[d]imidazol-1-yl) acetohydrazide derivatives

作　　者：李欢[1] 张思成[1] 胡静[2] 李子成[1] 赵瀛兰[2] 罗有福[2] 

机构地区：[1]四川大学化工学院,四川成都610065 [2]四川大学生物治疗国家重点实验室,四川成都610041

出　　处：《化学研究与应用》2014年第5期667-673,共7页Chemical Research and Application

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,1H 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.

关 键 词：苯并咪唑衍生物 乙酰腙 抗肿瘤活性 合成 

分 类 号：O626.2[理学—有机化学]