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1: Bioorg Med Chem Lett. 2007 Dec 1;17(23):6579-83. Epub 2007 Sep 25.
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2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.

Adams DR, Abraham A, Asano J, Breslin C, Dick CA, Ixkes U, Johnston BF, Johnston D, Kewnay J, Mackay SP, MacKenzie SJ, McFarlane M, Mitchell L, Spinks D, Takano Y.

Department of Chemistry, School of Engineering & Physical Sciences, Heriot-Watt University, Edinburgh EH14 4AS, UK. D.R.Adams@hw.ac.uk

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.

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PMID: 17931864 [PubMed - indexed for MEDLINE]