Discovery of 5-[[4-[(2, 3-Dimethyl-2 H-indazol-6-yl) methylamino]-2-pyrimidinyl] amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular …

…, RM Crosby, RG Davis-Ward, AH Epperly…

Index: Harris, Philip A.; Boloor, Amogh; Cheung, Mui; Kumar, Rakesh; Crosby, Renae M.; Davis-Ward, Ronda G.; Epperly, Andrea H.; Hinkle, Kevin W.; Hunter III, Robert N.; Johnson, Jennifer H.; Knick, Victoria B.; Laudeman, Christopher P.; Luttrell, Deirdre K.; Mook, Robert A.; Nolte, Robert T.; Rudolph, Sharon K.; Szewczyk, Jerzy R.; Truesdale, Anne T.; Veal, James M.; Wang, Liping; Stafford, Jeffrey A. Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4632 - 4640

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Citation Number: 195

Abstract

Inhibition of the vascular endothelial growth factor (VEGF) signaling pathway has emerged as one of the most promising new approaches for cancer therapy. We describe herein the key steps starting from an initial screening hit leading to the discovery of pazopanib, N 4-(2, 3-dimethyl-2 H-indazol-6-yl)-N 4-methyl-N 2-(4-methyl-3-sulfonamidophenyl)-2, 4- pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical ...