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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。
Aim To synthesize a novel aryl urea inhibitor Raf kinase and evaluate its antitumor activity. Methods Sorafenib 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. The anti-tumor activity was evaluated by MTT assay. Results Eleven new target compounds were synthesized, two of which showed significant anti-tumor activity in vitro. Conclusion The target compounds with good anti-tumor activity are intended to be further evaluated and modified as drug candidates.