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PDBsum entry 3cjg
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References listed in PDB file
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Key reference
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Title
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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.
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Authors
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P.A.Harris,
A.Boloor,
M.Cheung,
R.Kumar,
R.M.Crosby,
R.G.Davis-Ward,
A.H.Epperly,
K.W.Hinkle,
R.N.Hunter,
J.H.Johnson,
V.B.Knick,
C.P.Laudeman,
D.K.Luttrell,
R.A.Mook,
R.T.Nolte,
S.K.Rudolph,
J.R.Szewczyk,
A.T.Truesdale,
J.M.Veal,
L.Wang,
J.A.Stafford.
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Ref.
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J Med Chem, 2008,
51,
4632-4640.
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PubMed id
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Abstract
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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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