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

…, U Ixkes, BF Johnston, D Johnston, J Kewnay…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6579 - 6583

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被引用次数: 22

摘要

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 3–60μM IC50s for PTP1B inhibition in an Sf9 cell-based assay.