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Resumo(s)
Vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase is involved in cancer and in angiogenesis. Herein, we report the synthesis of novel1-aryl-3-[2-, 3- or 4-{thieno[3,2-b ]pyridin-7-ylthio) phenyl]ureas as VEGFR2 inhibitors by promoting the regioselective attack of the thiol group of the 4-aminothiophenol in the chlorine
nucleophilic displacement on 7-chlorothieno[3,2-b]pyridine 1, obtaining
the aminated compounds Za- c. These were reacted with
arylisocyanates to give the corresponding 1,3-diarylureas 3a-c, 4a-c
and Sa-c (see scheme).
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Citação
Peixoto, Daniela; Queiroz, Maria João; Abreu, Rui M.V.; Froufe, Hugo; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R. (2012). Synthesis of novel 1-aryl-3-[2,3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas and evaluation as VEGFR2 tyrosine kinase inhibitors. In XXIInd International Symposium on Medicinal Chemistry. Berlin