2-(Quinazolin-4-ylamino)-[1, 4] benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2

…, R Nilakantan, J Marini, M Ravi, K Cheung…

Index: Wissner, Allan; Floyd, M. Brawner; Johnson, Bernard D.; Fraser, Heidi; Ingalls, Charles; Nittoli, Thomas; Dushin, Russell G.; Discafani, Carolyn; Nilakantan, Ramaswamy; Marini, Joseph; Ravi, Malini; Cheung, Kinwang; Tan, Xingzhi; Musto, Sylvia; Annable, Tami; Siegel, Marshall M.; Loganzo, Frank Journal of Medicinal Chemistry, 2005 , vol. 48, # 24 p. 7560 - 7581

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Citation Number: 61

Abstract

A series of 2-(quinazolin-4-ylamino)-[1, 4] benzoquinone derivatives that function as potent covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2 (VEGFR-2) has been prepared by ceric ammonium nitrate oxidation of substituted (2, 5-dimethoxyphenyl)(6, 7-disubstituted-quinazolin-4-yl) amines and by displacement of the chlorine atom of substituted 2-chloro-5-(6, 7-disubstituted-quinazolin- ...