Synthesis and biological evaluation of novel N, N'-disubstituted urea and thiourea derivatives as potential anti-melanoma agents |
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Authors: | Li Qing-Shan Lv Peng-Cheng Li Huan-Qiu Lu Xiang Li Zi-Lin Ruan Ban-Feng Zhu Hai-Liang |
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Affiliation: | State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China. |
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Abstract: | 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. |
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