Affordable Access

deepdyve-link deepdyve-link
Publisher Website

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.

Authors
  • And 1 more
Type
Published Article
Journal
Journal of Medicinal Chemistry
1520-4804
Publisher
American Chemical Society
Publication Date
Volume
51
Issue
15
Pages
4632–4640
Identifiers
DOI: 10.1021/jm800566m
PMID: 18620382
Source
Medline
License
Unknown

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-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.

Statistics

Seen <100 times