Publicação
Heteroarylether 1,3-diarylureas in the thieno[3,2-d]pyrimidine series as VEGFR2 tyrosine Kinase inhibitors: synthesis, docking studies, enzymatic and cellular assays
| Resumo: | A number of thienopyrimidines derivatives have shown potent YEGFR2 (Vascular Endothelium Growth Factor Receptor2) inhibition activity [ 1]. YEGF is a surrogate marker of angiogenesis that activates VEGFR2 in endothelial cells. VEGF induces proliferation, migration and anastomosis of these cells. Here we present the synthesis of new l-aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas, by reaction of 4-aminophenol with 4-chlorothieno[3,2-d]pyrimidine giving compound 1, which was reacted with arylisocyanates to give the corresponding I ,3-diarylureas 2a-c (Scheme). |
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| Autores principais: | Queiroz, Maria João R.P. |
| Outros Autores: | Peixoto, Daniela; Soares, Pedro; Abreu, Rui M.V.; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R.; Costa, Raquel; Soares, Raquel |
| Ano: | 2012 |
| País: | Portugal |
| Tipo de documento: | documento de conferência |
| Tipo de acesso: | acesso aberto |
| Instituição associada: | Instituto Politécnico de Bragança |
| Idioma: | inglês |
| Origem: | Biblioteca Digital do IPB |
| Resumo: | A number of thienopyrimidines derivatives have shown potent YEGFR2 (Vascular Endothelium Growth Factor Receptor2) inhibition activity [ 1]. YEGF is a surrogate marker of angiogenesis that activates VEGFR2 in endothelial cells. VEGF induces proliferation, migration and anastomosis of these cells. Here we present the synthesis of new l-aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas, by reaction of 4-aminophenol with 4-chlorothieno[3,2-d]pyrimidine giving compound 1, which was reacted with arylisocyanates to give the corresponding I ,3-diarylureas 2a-c (Scheme). |
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