Bulletin of the Korean Chemical Society · 2008 · 16 citations · 10 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyDrug DesignDrug DiscoveryMelanoma PharmacotherapyTyrosine Kinase InhibitorsAntiproliferative AgentsAntiproliferative Drug ActionMedicinal Chemistry ApplicationsPhenyl Ring ReplacementPhenyl Ring Substitution EffectsPyrimidine AnalogsPyrimidine Analogues
The synthesis of a new series of diaryl ureas having a pyrr2,3-pyrimidine scaffold is reported here. The in vitro antiproliferative activities of these diaryl derivatives against human melanoma cell line A375 were tested and the effect of substituents on the phenyl ring was investigated. The para substituted compounds la-g showed superior or similiar activity to Sorafenib against the A375 cell line. Among these compounds, Ic-e showed excellent activity against A375 compared with Sorafenib, a multi-kinase inhibitor.
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