Synthesis and biological evaluation of novel N, N′-disubstituted urea and thiourea derivatives as potential anti-melanoma agents

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 (IC₅₀ = 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.

Keywords::

• Melanoma
• ERK
• phosphorylation
• urea
• thiourea

Acknowledgement

Qing-Shan Li and Peng-Cheng Lv have contributed equally to the work.

Declaration of interest

This work was supported by Jiangsu National Science Foundation (No. BK2009239).