Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-b enzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.,Journal of Medicinal Chemistry

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Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-b enzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2008 Aug 14 , DOI: 10.1021/jm800566m
Philip A. Harris ₁ , Amogh Boloor ₁ , Mui Cheung ₁ , Rakesh Kumar ₁ , Renae M. Crosby ₁ , Ronda G. Davis-Ward ₁ , Andrea H. Epperly ₁ , Kevin W. Hinkle ₁ , Robert N. Hunter ₁ , Jennifer H. Johnson ₁ , Victoria B. Knick ₁ , Christopher P. Laudeman ₁ , Deirdre K. Luttrell ₁ , Robert A. Mook ₁ , Robert T. Nolte ₁ , Sharon K. Rudolph ₁ , Jerzy R. Szewczyk ₁ , Anne T. Truesdale ₁ , James M. Veal ₁ , Liping Wang ₁ , Jeffrey A. Stafford ₁

Affiliation

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-sulfonamidopheny l)-2,4-pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical development for renal-cell cancer and other solid tumors.

中文翻译：

5-[[4-[（2,3-二甲基-2H-吲唑-6-基）甲基氨基] -2-嘧啶基]氨基] -2-甲基-b烯基磺酰胺（Pazopanib）的发现，一种新型有效的血管内皮细胞生长因子受体抑制剂。

血管内皮生长因子（VEGF）信号通路的抑制已成为最有前途的癌症治疗新方法之一。我们在此描述了关键步骤，这些步骤从最初的筛选命中开始，导致发现帕唑帕尼，N（4）-（2,3-二甲基-2H-吲唑-6-基）-N（4）-甲基-N（2 ）-（4-甲基-3-磺酰胺基吗啉1）-2,4-嘧啶二胺，一种有效的泛VEGF受体（VEGFR）抑制剂，正在临床开发中用于肾细胞癌和其他实体瘤。

更新日期：2017-01-31

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