Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Published
Journal Article
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-2H-indazol-6-yl)-N(4)-methyl-N(2)-(4-methyl-3-sulfonamidophenyl)-2,4-pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical development for renal-cell cancer and other solid tumors.
Full Text
Duke Authors
Cited Authors
- Harris, PA; Boloor, A; Cheung, M; Kumar, R; Crosby, RM; Davis-Ward, RG; Epperly, AH; Hinkle, KW; Hunter, RN; Johnson, JH; Knick, VB; Laudeman, CP; Luttrell, DK; Mook, RA; Nolte, RT; Rudolph, SK; Szewczyk, JR; Truesdale, AT; Veal, JM; Wang, L; Stafford, JA
Published Date
- August 2008
Published In
Volume / Issue
- 51 / 15
Start / End Page
- 4632 - 4640
PubMed ID
- 18620382
Pubmed Central ID
- 18620382
Electronic International Standard Serial Number (EISSN)
- 1520-4804
International Standard Serial Number (ISSN)
- 0022-2623
Digital Object Identifier (DOI)
- 10.1021/jm800566m
Language
- eng