3-芳香Shiff碱-5-氟吲哚-2酮衍生物的设计、合成与活性研究

Synthesis and biological evaluation of 3-aromatic Shiff base-5-fluoroindol-2-one derivatives

摘要:
在5-氟吲哚-2-酮的母体结构基础上, 选用13个已上市或处于临床研究阶段的多靶点酪氨酸激酶抑制剂的结构片段, 设计合成了11个3-芳香Shiff碱吲哚-2-酮衍生物。11个目标化合物的结构经¹H NMR、MS及元素分析确证。采用MTT法测试所合成化合物的体外抗肿瘤活性, 结果表明, 大多数化合物具有一定的抗癌作用, 其中化合物1b、1g、1i及1h的抗癌活性优于或相当于阳性对照。

Abstract:
Based on the structure of 5-fluoroindol-2-one and fragments from thirteen multi-target tyrosine kinase inhibitors which have been marketed or in the phase of clinical research, eleven 3-aromatic Shiff base- 5-fluoroindol-2-one derivatives were designed and synthesized. Their structures were identified by ¹H NMR, MS and elemental analysis. In vitro antitumor bioactivities evaluation was done by MTT method. It was shown that most of synthesized compounds had antitumor activities and compounds 1b, 1g, 1i and 1h were better than or equal to the antitumor activity of positive control.