在已上市的多靶点小分子靶向抗肿瘤药sorafenib的基础上,设计合成了16个4-[4-(2-甲胺酰基吡啶)]氧苯基芳香硫脲衍生物。16个目标化合物的结构经1H NMR、MS及元素分析确证。采用四氮唑盐(MTT)法测试了所合成化合物的体外抗肿瘤活性,结果表明所合成的化合物均具有一定的抗肿瘤活性,其中化合物1a、1d、1i及1j的抗肿瘤活性优于或相当于阳性对照sorafenib。 Sixteen 4- [4- (2-carbamyl pyridyl)] oxyphenylthiourea derivatives were designed and synthesized on the basis of the sorafenib, a multi-target small molecule targeted antitumor agent already on the market. The structure of 16 target compounds was confirmed by 1H NMR, MS and elemental analysis. The antitumor activity of the synthesized compounds was tested by MTT method. The results showed that the synthesized compounds all had certain antitumor activities. The antitumor activity of compounds 1a, 1d, 1i and 1j was better than that of Equivalent to the positive control sorafenib.