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.
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, 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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Chicago
ICMJE
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NLM
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, 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. 2008 Aug 14;51(15):4632–40.
Harris, Philip A., 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, vol. 51, no. 15, Aug. 2008, pp. 4632–40. Pubmed, doi: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.
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