目的合成新型芳基脲类血管内皮生长因子受体抑制剂并评价其抗肿瘤活性。方法以Tivozanib为先导化合物进行结构改造,设计合成系列芳基脲类衍生物,1H-NMR和ESI-MS鉴定目标物结构,并用MTT法进行体外抑制肿瘤细胞增殖活性评价。结果合成10个新目标化合物,其中7个表现出显著的体外抑制肿瘤细胞增殖活性。结论目标化合物体外活性好,值得进一步研究。 OBJECTIVE To synthesize a novel aryl urea-based vascular endothelial growth factor receptor inhibitor and evaluate its anti-tumor activity. Methods Tivozanib was used as the lead compound for structural transformation. A series of aryl urea derivatives were designed and synthesized. The structures of the target compounds were identified by 1H-NMR and ESI-MS. MTT assay was used to evaluate the proliferation activity of tumor cells in vitro. Results Ten new target compounds were synthesized, of which seven showed significant inhibition of tumor cell proliferative activity in vitro. Conclusion The target compound has good in vitro activity and deserves further study.