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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
    Harris, Philip A; Boloor, Amogh; Cheung, Mui; Kumar, Rakesh; Crosby, Renae M; Davis-Ward, Ronda G; Epperly, Andrea H; Hinkle, Kevin W; Hunter, 3rd, Robert N; Johnson, Jennifer H; Knick, Victoria B; Laudeman, Christopher P; Luttrell, Deirdre K; Mook, Robert A; Nolte, Robert T; Rudolph, Sharon K; Szewczyk, Jerzy R; Truesdale, Anne T; Veal, James M; Wang, Liping; Stafford, Jeffrey A

    Journal of medicinal chemistry, 08/2008, Letnik: 51, Številka: 15
    Journal Article

    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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