Nitroarylhydroxymethylphosphonic acids as inhibitors of CD45

被引：22

作者：

Beers, SA ^{[1
]}

Malloy, EA ^{[1
]}

Wu, W ^{[1
]}

Wachter, MP ^{[1
]}

Gunnia, U ^{[1
]}

Cavender, D ^{[1
]}

Harris, C ^{[1
]}

Davis, J ^{[1
]}

Brosius, R ^{[1
]}

Pellegrino-Gensey, JL ^{[1
]}

Siekierka, J ^{[1
]}

机构：

[1] RW Johnson Pharmaceut Res Inst, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 12期

关键词：

D O I：

10.1016/S0968-0896(97)00174-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of nitroarylhydroxymethylphosphonic acids was synthesized and evaluated as inhibitors of CD45. It was discovered that both the alpha hydroxy and nitro groups are essential for activity. Potency is enhanced by the addition of a large lipophilic group on the aryl ring adjacent to the phosphonic acid moiety. Kinetics studies have shown that these compounds are competitive inhibitors and thus bind at the active site of this enzyme. (C) 1997 Elsevier Science Ltd.

引用

页码：2203 / 2211

页数：9

共 19 条

[1] REQUIREMENT FOR INTRINSIC PROTEIN TYROSINE KINASE IN THE IMMEDIATE AND LATE ACTIONS OF THE EGF RECEPTOR [J].