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PDBsum entry 3cth
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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 orally active pyrrolopyridine- And aminopyridine-Based met kinase inhibitors.
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Authors
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Z.W.Cai,
D.Wei,
G.M.Schroeder,
L.A.Cornelius,
K.Kim,
X.T.Chen,
R.J.Schmidt,
D.K.Williams,
J.S.Tokarski,
Y.An,
J.S.Sack,
V.Manne,
A.Kamath,
Y.Zhang,
P.Marathe,
J.T.Hunt,
L.J.Lombardo,
J.Fargnoli,
R.M.Borzilleri.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
3224-3229.
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PubMed id
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Abstract
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A series of acylurea analogs derived from pyrrolopyridine and aminopyridine
scaffolds were identified as potent inhibitors of Met kinase activity. The SAR
at various positions of the two kinase scaffolds was investigated. These studies
led to the discovery of compounds 3b and 20b, which demonstrated favorable
pharmacokinetic properties in mice and significant antitumor activity in a human
gastric carcinoma xenograft model.
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