α,α-difluoro-β-ketophosphonates as potent inhibitors of protein tyrosine phosphatase 1B

被引：52
作者：
Li, XF [1 ]
Bhandari, A [1 ]
Holmes, CP [1 ]
Szardenings, AK [1 ]
机构：
[1] Affymax Inc, Palo Alto, CA 94304 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 16期
关键词：
D O I：
10.1016/j.bmcl.2004.05.082
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of inhibitors that contain an aryl alpha,alpha-difluoro-beta-ketophosphonate group has been synthesized and evaluated against protein tyrosine phosphatase 1B. These compounds exhibit strong inhibitory activity, the best of which has a K-i value of 0.17 muM. These results demonstrate that aryl alpha,alpha-difluoro-beta-ketophosphonates are powerful phosphotyrosine mimetics for the development of potent PTP inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.
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页码：4301 / 4306
页数：6
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