Heteroarylether 1,3-diarylureas in the thieno[3,2-d]pyrimidine series as VEGFR2 tyrosine Kinase inhibitors: synthesis, docking studies, enzymatic and cellular assays

Queiroz, Maria João R.P.; Peixoto, Daniela; Soares, Pedro; Abreu, Rui M.V.; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R.; Costa, Raquel; Soares, Raquel

http://hdl.handle.net/10198/7357

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Authors

Queiroz, Maria João R.P.

Ferreira, Isabel C.F.R.

Costa, Raquel

Soares, Raquel

Abstract(s)

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).

URI

http://hdl.handle.net/10198/7357

Citation

Queiroz, Maria-João R.P.; Peixoto, Daniela; Soares, Pedro; Abreu, Rui M.V.; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R.; Costa, Raquel; Soares, Raquel (2012). Heteroarylether 1,3-diarylureas in the thieno[3,2-d]pyrimidine series as VEGFR2 tyrosine Kinase inhibitors: synthesis, docking studies, enzymatic and cellular assays. In 48th International conference on Medicinal Chemistry. Interfacing Chemical Biology and Drug Discovery. Poitiers.