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…
文献索引：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
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 ...
