应用化学 ›› 2010, Vol. 27 ›› Issue (09): 1017-1020.DOI: 10.3724/SP.J.1095.2010.90838

• 研究论文 • 上一篇    下一篇

联苯并咪唑化合物的合成、表征与抗癌活性

李建晓1,毛郑州1,梅文杰2,汪朝阳1*   

  1. (1.华南师范大学化学与环境学院 广州 510006;2.广东药学院医药化工学院 广州)
  • 收稿日期:2009-12-11 修回日期:2010-01-16 出版日期:2010-09-10 发布日期:2010-09-10
  • 通讯作者: 汪朝阳,男,博士,教授; E-mail:wangwangzhaoyang@tom.com; 研究方向:有机合成与功能高分子材料
  • 基金资助:
    国家自然科学基金(20772035)广东省自然科学基金(5300082)广东药学院中青年骨干教师培养基金广东省科技计划项目(2007B031513004)资助项目

Synthesis and Characterization of Bisbenzimidazoles and their Anti-cancer Activity

LI Jian-Xiao1, MAO Zheng-Zhou1, MEI Wen-Jie2, WANG Zhao-Yang1*   

  1. (1.School of Chemistry and Environment,South China Normal University,Guangzhou 510006;
    2.School of Chemistry and Chemical Engineeing,Guangdong Pharmaceutical University,Guangzhou)
  • Received:2009-12-11 Revised:2010-01-16 Published:2010-09-10 Online:2010-09-10

摘要:

以联苯四胺、芳香醛为原料,DMF为溶剂,KI为催化剂,在空气存在下回流反应,合成了6种新的联苯并咪唑化合物,产率较高(58.4%~98.0%),其结构用IR、1H NMR、13C NMR、MS、元素分析等测试技术进行了表征。 适宜的合成条件是:反应温度150 ℃,反应时间12 h。 初步测试表明,目标化合物对培养人肝癌Bel-7402细胞生长有一定抑制活性。

关键词: 联苯并咪唑, 合成, 表征, 抗癌活性

Abstract:

Using DMF as solvent, 3,3′-diaminobenzidine and aromatic aldehydes as starting materials, and KI as catalyst, six new bisbenzimidazoles were synthesized in the presence of air. The structures of the compounds were characterized by means of FTIR, 1H NMR, 13C NMR, MS and elemental analysis. The optimal synthetic conditions were investigated. When the temperature was 150 ℃ and the reaction time was 12 h, the six compounds were obtained with yields in the range of 58.4% to 98.0%. The new method with readily available catalyst is advantageous to conventional synthetic process of bisbenzimidazoles due to its less steps, simpler operations, easier postprocessings and higher yields. The anti-tumor activities of the target compounds were preliminarily examined via MTT method on Bel-7402 cell in vitro, and they exhibited certain inhibition activities.

Key words: Bisbenzimidazoles, Synthesis, Characterization, Anti-cancer activity

中图分类号: