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

Journal Article · Mon May 18 00:00:00 EDT 2009 · J. Med. Chem.

DOI:https://doi.org/10.1021/jm800566m· OSTI ID:1007084

Harris, Philip A; Boloor, Amogh; Cheung, Mui; Kumar, Rakesh; Crosby, Renae M; Davis-Ward, Ronda G; Epperly, Andrea H; Hinkle, Kevin W; 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 ^[1]

---

1. GSKNC

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{sup 4}-(2,3-dimethyl-2H-indazol-6-yl)-N{sup 4}-methyl-N{sup 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.

• Research Organization: Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
• Sponsoring Organization: USDOE
• OSTI ID: 1007084
• Journal Information: J. Med. Chem., Vol. 51, Issue (15) ; 08, 2008; ISSN 0022-2623
• Country of Publication: United States
• Language: ENGLISH

Related Subjects

60 APPLIED LIFE SCIENCES
GROWTH FACTORS
RECEPTORS
INHIBITION
SULFONAMIDES
NEOPLASMS
THERAPY