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Abstract(s)
When over expressed or mutated, protein tyrosine kinases become potent oncoproteins that cause deregulated cell growth angiogenesis and metastasis. Because of these characteristics, they are targets for small molecule inhibitors in the treatment of cancer. Recently some thieno[3,2-c]pyridine 1,3-diarylurea derivatives were prepared as VEGFR-2 (vascular endothelium growth factor receptor-2) inhibitors.1 Here we present the synthesis of methyl 3-[4-(3-arylureido)phenylamino]thieno[3,2-b]pyridine-2-carboxylates 2 in excellent yields, by reaction of the methyl 3-(4-aminophenylamino)thieno[3,2-b]pyridine-2-carboxylate 1, prepared also by us, with different arylisocyanates (Scheme).
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Citation
Peixoto, Daniela; Calhelha, Ricardo C.; Dias, Sofia; Froufe, Hugo; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Queiroz, Maria-João R.P. (2011). Methyl 3-[4-(3-arylureido)phenylamino]thieno[3,2-b]pyridine-2-carboxylates as potential inhibitors of VEGFR-2: synthesis and molecular modelling studies. In 2nd Iberic Meeting on Medicinal Chemistry: G Protein-Coupled Receptors and Enzymes in Drug Discovery. Porto