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Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) is the major receptor of the angiogenic effects when
linked to VEGF released by tumors. It has a well known role as a transmembrane receptor activating multiple
signaling pathways of proliferation and migration of endothelial cells [1], thus leading to the formation and the
expansion of new blood vessels (vasculogenesis and angiogenesis) towards the tumor [2]. Therefore, several
approaches have been developed to inhibit VEGFR activation and signaling [3].
Some thienopyridine derivatives have already been shown to be inhibitors of the tyrosine kinase domain of
VEGFR2 preventing its activation [4]. Herein, we describe the synthesis of new N-[3-(thieno[3,2-b]pyridine-7 -ylthio )phenyl]benzamides, suggested by rational design as potential inhibitors of this domain, either
through a Cu-catalyzed C-N coupling of a brominated di(hetero)arylthioether thieno[3,2-b]pyridine with
benzamides, or through a reaction of an aminated di(hetero )arylthioether thieno[3,2-b ]pyridine with benzoyl chlorides, as presented below. The inhibition of the tyrosine kinase domain of VEGFR2 by the synthesized compounds will be evaluated by
enzymatic and biomolecular assays using VEGF-stimulated Human Umbilical Vein Endothelial Cells
(HUVECs).
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Queiroz, Maria João R.P.; Begouin, Agathe; Campos, Joana F.; Peixoto, Daniela; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R. (2013). Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as potential inhibitors of VEGFR2 using rational design. In 49th International Conference on Medicinal Chemistry (RICT 2013). Nice