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Angiogenesis is the process of new blood vessel formation from pre-existing vascular networks by capillary sprouting, and plays an important role in the pathogenesis of several disorders including cancer, proliferative retinopathies and rheumatoid arthritis. A key regulatory pathway of angiogenesis is mediated by the vascular endothelial growth factor (VEGF) and its cell membrane tyrosine kinase receptor VEGFR-2 (also know as KDR kinase) [1]. Several VEGFR-2 inhibitors have emerged as promising anti-angiogenic agents for possible treatment against a wide variety of cancers including: sorafenib, sunitinib, and pazopanib, that have been approved for the treatment of advanced renal cell carcinoma. Several scaffolds have been studied for anti-VEGFR-2 activity as thieno[3,2-b]pyridines [2].
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Abreu, Rui M.V.; Froufe, Hugo J.C.; Ferreira, Isabel C.F.R.; Queiroz, Maria-João R.P. (2011). Rational design of thieno[3,2-b]pyridines as potential new VEGFR-2 inhibitors based on improved docking scores. In XII Encontro Nacional da Sociedade Portuguesa de Química: 100 anos de Química em Portugal. Braga