索拉非尼类似物的合成和体外抗肿瘤活性研究

Synthesis and in vitro cytotoxic activities of sorafenib derivatives

本研究以索拉非尼为先导化合物,对其结构进行改造,合成了一系列酰肼羧酸类化合物。用MTT法对目标化合物进行了体外抗肿瘤活性筛选,结果显示部分化合物对测试肿瘤细胞的抑制活性优于阳性对照药索拉非尼,其中化合物7c对ACHN、HCT116、MDA-MB-231的IC50值分别为9.01、4.97和6.61μmol·L-1。

A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 μ mol·L-1. Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7e demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC 50 values of 9.01, 4.97, 6.61 μmol·L-1, respectively.