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 Inhib

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• 作者：Philip A. Harris ; Amogh Boloor ; Mui Cheung ; Rakesh Kumar ; Renae M. Crosby ; Ronda G. Davis-Ward ; Andrea H. Epperly ; Kevin W. Hinkle ; Robert N. Hunter ; ; Jennifer H. Johnson ; Victoria B. Knick ; Christop
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：August 14, 2008
• 年：2008
• 卷：51
• 期：15
• 页码：4632-4640
• 全文大小：254K
• 年卷期：v.51,no.15(August 14, 2008)
• ISSN：1520-4804

文摘

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, N⁴-(2,3-dimethyl-2H-indazol-6-yl)-N⁴-methyl-N²-(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.