新型苯并咪唑衍生物的合成及生物活性研究  

Synthesis and evaluation on biological activity of novel benzimidazole derivatives

作　　者：张涛[1] 王宁宇[2] 夏勇[2] 马丽芳[1] 余洛汀[1,2] 

机构地区：[1]四川大学化工学院,四川成都610064 [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》2012年第7期1136-1140,共5页Chemical Research and Application

摘　　要：以取代苯酚为原料,合成8个新型的2-苯氧甲基苯并咪唑类化合物,通过1H-NMR和HRMS确认其结构。MTT法测试其抗肿瘤活性,实验结果表明,大部分化合物具有较好的广谱抗肿瘤效果,其中化合物2h对大多数肿瘤细胞株的IC50值均达到了低微摩尔水平,对人胰腺癌(BxPC-3)的IC50达到3.6μM。试管二倍稀释法测试其抗菌活性,实验结果表明,目标化合物显示出抗菌活性,化合物2a对粪肠球菌和金黄色葡萄球菌的MIC达到16μg/mL。Eight 2-phenoxybenzimidazole derivatives were synthesized from substituted phenol.The structure of these compound were validated by 1H-nuclear magnetic resonance（1H-NMR）and high resolution mass spectrometer（HRMS）.The antitumor activity of these compounds were achieved by MTT test,while the antibacterial activity were obtained by tube double dilution method.All these compounds showed broad spectrum antitumor potency,especially,compound 2h exhibited good antitumor potency with IC50 values of low micromolar to all these cell lines and the IC50 values of 2h to human pancreatic cancer cell line（BxPC-3）was 3.6 μM.Meanwhile,most compounds displayed moderate antibacterial activity,especially,compound 2a inhibit E.faecalis and S.aureus with a MIC of 16 μg/mL.

关 键 词：苯并咪唑 抗菌 抗肿瘤 合成 

分 类 号：O626.3[理学—有机化学]