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PDBsum entry 3cwe
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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 [(3-Bromo-7-Cyano-2-Naphthyl)(difluoro)methyl]phosphonic acid, A potent and orally active small molecule ptp1b inhibitor.
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Authors
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Y.Han,
M.Belley,
C.I.Bayly,
J.Colucci,
C.Dufresne,
A.Giroux,
C.K.Lau,
Y.Leblanc,
D.Mckay,
M.Therien,
M.C.Wilson,
K.Skorey,
C.C.Chan,
G.Scapin,
B.P.Kennedy.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
3200-3205.
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PubMed id
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Abstract
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A series of quinoline/naphthalene-difluoromethylphosphonates were prepared and
were found to be potent PTP1B inhibitors. Most of these compounds bearing polar
functionalities or large lipophilic residues did not show appreciable oral
bioavailability in rodents while small and less polar analogs displayed moderate
to good oral bioavailability. The title compound was found to have the best
overall potency and pharmacokinetic profile and was found to be efficacious in
animal models of diabetes and cancer.
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