2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.

Article Details

Citation

Copy to clipboard

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

2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6579-83. Epub 2007 Sep 25.

PubMed ID

17931864 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
5-(2-Fluoro-5-{(1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]-1-propen-1-yl}phenyl)-1,2-oxazole-3-carboxylic acid	Tyrosine-protein phosphatase non-receptor type 1	IC 50 (nM)	110000	N/A	N/A	Details