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

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Assay
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Enzyme-Linked Immunosorbent Assay
  • Fluorescent Antibody Technique
  • Inhibitory Concentration 50
  • MAP Kinase Signaling System
  • Magnetic Resonance Spectroscopy
  • Melanoma, Experimental / drug therapy*
  • Melanoma, Experimental / pathology
  • Mice
  • Phosphorylation
  • Spectrometry, Mass, Electrospray Ionization
  • Thiourea / chemical synthesis
  • Thiourea / pharmacology
  • Thiourea / therapeutic use
  • Urea / chemical synthesis*
  • Urea / pharmacology*
  • Urea / therapeutic use


  • Urea
  • Thiourea