新型芳基脲类Raf激酶抑制剂的合成及抗肿瘤活性

Synthesis and Antitumor Activities of Alylurea Derivatives Asnovel Raf Kinase Inhibitors

目的合成新型芳基脲类Raf激酶抑制剂并评价其抗肿瘤活性。方法以索拉非尼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法进行体外抗肿瘤活性评价。结果合成11个新目标化合物,其中2个表现出显著的体外抗肿瘤活性。结论抗肿瘤活性好的目标化合物体拟作为候选药做进一步的评价和修饰。

Objective To synthesize novel aryl urea Raf kinase inhibitors and to study their antitumor activity.Methods With SoRafenib as the lead compound,eleven novel aryl urea compounds were designed, synthesized and characterized by ^1H-NMR and ESI-MS. Their antitumor activities were investigated by MTT methods.Results Eleven novel compounds were synthesized,two of which had better antitumor activities.Conclusion Target compourds with good antitumor activities can potentially serve as drug candidates for further evaluation and modification.