Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors

…, J Sechler, A Fuentes-Pesquera…

Index: Kuo, Gee-Hong; Prouty, Catherine; Wang, Aihua; Emanuel, Stuart; DeAngelis, Alan; Zhang, Yan; Song, Fengbin; Beall, Lawrence; Connolly, Peter J.; Karnachi, Prahba; Chen, Xin; Gruninger, Robert H.; Sechler, Jan; Fuentes-Pesquera, Angel; Middleton, Steven A.; Jolliffe, Linda; Murray, William V. Journal of Medicinal Chemistry, 2005 , vol. 48, # 15 p. 4892 - 4909

Full Text: HTML

Citation Number: 31

Abstract

There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth factor receptor-2 (VEGFR-2) will result in the reduction of angiogenesis and the suppression of tumor growth. Palladium-catalyzed CC bond, CN bond formation reactions were used to assemble various pyrazine-pyridine biheteroaryls as potent VEGFR-2 inhibitors. Among them, 4-{5-[6-(3-chloro-phenylamino)-pyrazin-2-yl]-pyridin-3-ylamino}- ...