Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the UGI four-component condensation

被引：25
|
作者：
Li, ZG [1 ]
Yeo, SL [1 ]
Pallen, CJ [1 ]
Ganesan, A [1 ]
机构：
[1] Natl Univ Singapore, Inst Mol & Cell Biol, Singapore 117609, Singapore
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 18期
关键词：
solid phase synthesis; phosphonic acids and derivs; enzyme inhibitors;
D O I：
10.1016/S0960-894X(98)00408-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A library of 108 alpha,alpha-difluoromethylenephosphonic acids was prepared by Ugi four-component condensation using Rink-NH(2) resin, 4-[(diethoxyphosphinyl)difluoromethyl]benzoic acid, and a set of 18 aldehydes and 6 isonitriles. Following resin cleavage, the diethylphosphonate esters were hydrolyzed with trimethylsilyl bromide to yield the free acids which were assayed for inhibition of PTF alpha, PTP beta and PTP epsilon. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2443 / 2446
页数：4
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