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Discovery of 5-[[4-[(2,3-Dimethyl-2 H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor
Open accessAbstract
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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Metadata
- Authors
- Harris, P. A., Boloor, A., Cheung, M., Kumar, R., Crosby, R. M., Davis-Ward, R. G., Epperly, A. H., Hinkle, K. W., Hunter, R. N., Johnson, J. H., Knick, V. B., Laudeman, C. P., Luttrell, D. K., Mook, R. A., Nolte, R. T., Rudolph, S. K., Szewczyk, J. R., Truesdale, A. T., Veal, J. M., Wang, L., & Stafford, J. A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-07-12
- Volume
- 51
- Issue
- 15
- Pages
- 4632-4640
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2035387891
- Cited by
- 352
- References
- 0
- FWCI
- 6.70
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Discovery of 5-[[4-[(2,3-Dimethyl-2 H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor. https://app.cochat.ai/papers/10.1021/jm800566m
- The paper
- Harris, P. A., Boloor, A., Cheung, M., Kumar, R., Crosby, R. M., Davis-Ward, R. G., Epperly, A. H., Hinkle, K. W., Hunter, R. N., Johnson, J. H., Knick, V. B., Laudeman, C. P., Luttrell, D. K., Mook, R. A., Nolte, R. T., Rudolph, S. K., Szewczyk, J. R., Truesdale, A. T., Veal, J. M., . . . Stafford, J. A. (2008). Discovery of 5-[[4-[(2,3-Dimethyl-2 H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm800566m
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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