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Bioorg Med Chem Lett ; 17(23): 6579-83, 2007 Dec 01.
Article in English | MEDLINE | ID: mdl-17931864

ABSTRACT

A new series of non-peptidic, mono-acid protein tyrosine phosphatase 1B (PTP1B) inhibitors has been identified by structure-based design. Compounds with 2-(indol-3-yl)- and 2-phenyl-3,3,3-trifluoro-2-hydroxypropionic acid core units targeted at the enzyme's primary site and a hydrophobic chlorophenylthiazole extension in its 2 degrees site exhibit 3-60microM IC(50)s for PTP1B inhibition in an Sf9 cell-based assay.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Propionates/chemistry , Propionates/classification , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Animals , Binding Sites , Cell Line , Enzyme Inhibitors/classification , Enzyme Inhibitors/metabolism , Ligands , Propionates/pharmacology , Protein Tyrosine Phosphatase, Non-Receptor Type 1/metabolism , Spodoptera/cytology
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