State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
J Enzyme Inhib Med Chem. 2012 Oct;27(5):708-14. doi: 10.3109/14756366.2011.608665. Epub 2011 Oct 10.
Two series of urea and thiourea derivatives (1a-11a, 1b-11b) have been synthesized; all the 22 compounds were reported for the first time. Their anti-proliferative activities against the melanoma cell line B16-F10 were evaluated. Among the compounds tested, compound 6b exhibited the most potent activity in melanoma cells growth inhibition (IC(50) = 0.33 μM). The bioassay tests showed that anti-proliferative activities of these novel compounds were possibly caused by inhibition of ERK1/2 phosphorylation level. Therefore, compound 6b can be a potential anti-melanoma agent and an inhibitor of ERK1/2 phosphorylation deserving further research.
已经合成了两个系列的脲和硫脲衍生物（1a-11a，1b-11b）；所有 22 种化合物均为首次报道。评估了它们对黑色素瘤细胞系 B16-F10 的抗增殖活性。在所测试的化合物中，化合物 6b 对黑色素瘤细胞生长抑制的活性最强（IC（50）=0.33 μM）。生物测定试验表明，这些新型化合物的抗增殖活性可能是通过抑制 ERK1/2 磷酸化水平引起的。因此，化合物 6b 可能是一种潜在的抗黑色素瘤药物和 ERK1/2 磷酸化抑制剂，值得进一步研究。
