Details

Autor(en) / Beteiligte

• Adams, David R.
• Abraham, Achamma
• Asano, Jun
• Breslin, Catherine
• Dick, Colin A.J.
• Ixkes, Ulrich
• Johnston, Blair F.
• Johnston, Derek
• Kewnay, Justin
• Mackay, Simon P.
• MacKenzie, Simon J.
• McFarlane, Morag
• Mitchell, Lee
• Spinks, Daniel
• Takano, Yasuo

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry, 2007-12, Vol.17 (23), p.6579-6583

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2007

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• A new series of protein tyrosine phosphatase 1B inhibitors with a 2-aryl-3,3,3-trifluoro-2-hydroxypropionic acid core unit targeted at the enzyme’s primary site and a hydrophobic chlorophenylthiazole extension in the 2° site exhibit low-μM inhibitory activity in cell-based assays. 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° site exhibit 3–60 μM IC 50s for PTP1B inhibition in an S f9 cell-based assay.