论文部分内容阅读
本文以索拉非尼为先导化合物进行结构改造,合成了一系列苄基脲类化合物。采用MTT法对目标化合物进行了体外抗肿瘤活性筛选,药理结果显示部分化合物对多种人肿瘤细胞的抑制作用与索拉非尼相当,其中化合物20和23分别针对HT-29和MX-1肿瘤细胞的抑制作用的IC50值达微摩尔水平,明显优于阳性对照药索拉非尼,尤其是酰胺部分含3-吡啶基的化合物20,不仅具有较强的抑制HT-29活性,其IC50值为3.82μmol·L-1,而且溶解度与索拉非尼相比有较明显的提高,值得进一步研究。
In this paper, Sorafenib as the lead compound for structural transformation, synthesis of a series of benzyl urea compounds. The target compounds were screened by MTT method in vitro. The pharmacological results showed that the inhibitory effect of some compounds on so many human tumor cells was comparable to that of sorafenib. Compounds 20 and 23 were respectively targeted against HT-29 and MX-1 tumors The IC50 value of cell inhibition reached micromolar level, which was significantly better than that of sorafenib positive control. Especially, the compound 20 with 3-pyridyl group in the amide moiety not only had a strong inhibitory activity on HT-29, but also had an IC50 value 3.82μmol·L-1, and the solubility of sorafenib compared with a more significant increase, it is worth further study.