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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。
In this study, sorafenib as the lead compound, its structure was modified, a series of hydrazide carboxylic acid compounds were synthesized. The antitumor activity of the target compounds was screened by MTT assay. The results showed that the inhibitory activity of some of the compounds on the tested tumor cells was better than that of the positive control sorafenib, and IC50 of compound 7c for ACHN, HCT116 and MDA-MB-231 The values were 9.01, 4.97 and 6.61 μmol·L-1, respectively.