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

被引：33

作者：

Adams, David R. ^{[1
]}

Abraham, Achamma ^{[1
]}

Asano, Jun ^{[2
]}

Breslin, Catherine ^{[4
]}

Dick, Colin A. J. ^{[3
]}

Ixkes, Ulrich ^{[1
]}

Johnston, Blair F. ^{[5
]}

Johnston, Derek ^{[3
]}

Kewnay, Justin ^{[3
]}

Mackay, Simon P. ^{[5
]}

MacKenzie, Simon J. ^{[3
]}

McFarlane, Morag ^{[4
]}

Mitchell, Lee ^{[3
]}

Spinks, Daniel ^{[3
]}

Takano, Yasuo ^{[2
]}

机构：

[1] Heriot Watt Univ, Sch Engn & Phys Sci, Dept Chem, Edinburgh EH14 4AS, Midlothian, Scotland

[2] Kyorin Pharmaceut Co Ltd, Discovery Res Labs, Tochigi 3290114, Japan

[3] Kyorin Scotland Res Labs, Glasgow G20 OXA, Lanark, Scotland

[4] Scottish Biomed, Glasgow G20 OXA, Lanark, Scotland

[5] Univ Strathclyde, Strathclyde Inst Pharm & Biomed Sci, Glasgow G4 0NR, Lanark, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2007.09.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

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 degrees site exhibit 3-60 mu M IC(50)s for PTP1B inhibition in an Sf9 cell-based assay. (c) 2007 Elsevier Ltd. All rights reserved.

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收藏

页码：6579 / 6583

页数：5

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