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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.

Publication ,  Journal Article
Harris, PA; Boloor, A; Cheung, M; Kumar, R; Crosby, RM; Davis-Ward, RG; Epperly, AH; Hinkle, KW; Hunter, RN; Johnson, JH; Knick, VB; Mook, RA ...
Published in: J Med Chem
August 14, 2008

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.

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Published In

J Med Chem

DOI

EISSN

1520-4804

Publication Date

August 14, 2008

Volume

51

Issue

15

Start / End Page

4632 / 4640

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Sulfonamides
  • Receptors, Vascular Endothelial Growth Factor
  • Pyrimidines
  • Protein Kinase Inhibitors
  • Neoplasms
  • Molecular Structure
  • Models, Molecular
  • Mice
  • Medicinal & Biomolecular Chemistry
 

Citation

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Harris, P. A., Boloor, A., Cheung, M., Kumar, R., Crosby, R. M., Davis-Ward, R. G., … Stafford, J. A. (2008). 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. J Med Chem, 51(15), 4632–4640. https://doi.org/10.1021/jm800566m
Harris, Philip A., Amogh Boloor, Mui Cheung, Rakesh Kumar, Renae M. Crosby, Ronda G. Davis-Ward, Andrea H. Epperly, et al. “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.J Med Chem 51, no. 15 (August 14, 2008): 4632–40. https://doi.org/10.1021/jm800566m.
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. 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. J Med Chem. 2008 Aug 14;51(15):4632–4640.
Journal cover image

Published In

J Med Chem

DOI

EISSN

1520-4804

Publication Date

August 14, 2008

Volume

51

Issue

15

Start / End Page

4632 / 4640

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Sulfonamides
  • Receptors, Vascular Endothelial Growth Factor
  • Pyrimidines
  • Protein Kinase Inhibitors
  • Neoplasms
  • Molecular Structure
  • Models, Molecular
  • Mice
  • Medicinal & Biomolecular Chemistry