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PDBsum entry 4knb
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Contents |
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273 a.a.
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256 a.a.
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271 a.a.
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247 a.a.
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References listed in PDB file
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Key reference
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Title
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Novel 6-Aminofuro[3,2-C]pyridines as potent, Orally efficacious inhibitors of cmet and ron kinases.
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Authors
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A.G.Steinig,
A.H.Li,
J.Wang,
X.Chen,
H.Dong,
C.Ferraro,
M.Jin,
M.Kadalbajoo,
A.Kleinberg,
K.M.Stolz,
P.A.Tavares-Greco,
T.Wang,
M.R.Albertella,
Y.Peng,
L.Crew,
J.Kahler,
J.Kan,
R.Schulz,
A.Cooke,
M.Bittner,
R.W.Turton,
M.Franklin,
P.Gokhale,
D.Landfair,
C.Mantis,
J.Workman,
R.Wild,
J.Pachter,
D.Epstein,
M.J.Mulvihill.
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Ref.
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Bioorg Med Chem Lett, 2013,
23,
4381-4387.
[DOI no: ]
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PubMed id
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Abstract
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A series of novel 6-aminofuro[3,2-c]pyridines as kinase inhibitors is described,
most notably, OSI-296 (6). We discuss our exploration of structure-activity
relationships and optimization leading to OSI-296 and disclose its
pharmacological activity against cMET and RON in cellular assays. OSI-296 is a
potent and selective inhibitor of cMET and RON kinases that shows in vivo
efficacy in tumor xenografts models upon oral dosing and is well tolerated.
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