title: 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 (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.
authors: State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
authors: Qing-Shan
authors: QS
authors: Li
authors: Peng-Cheng
authors: PC
authors: Lv
authors: Huan-Qiu
authors: HQ
authors: Li
authors: Xiang
authors: X
authors: Lu
authors: Zi-Lin
authors: ZL
authors: Li
authors: Ban-Feng
authors: BF
authors: Ruan
authors: Hai-Liang
authors: HL
authors: Zhu
mesh_terms: D000818:Animals; D001681:Biological Assay; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004797:Enzyme-Linked Immunosorbent Assay; D005455:Fluorescent Antibody Technique; D020128:Inhibitory Concentration 50; D020935:MAP Kinase Signaling System; D009682:Magnetic Resonance Spectroscopy; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D010766:Phosphorylation; D021241:Spectrometry, Mass, Electrospray Ionization; D013890:Thiourea / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D014508:Urea / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D014508:Urea; D013890:Thiourea