STRUCTURAL INFLUENCES OF STYRYL-BASED INHIBITORS ON EPIDERMAL GROWTH-FACTOR RECEPTOR AND P56LCK TYROSINE-SPECIFIC PROTEIN-KINASES

被引：10

作者：

BURKE, TR

LI, ZH

BOLEN, JB

MARQUEZ, VE

机构：

[1] NCI,TUMOR VIRUS BIOL LAB,BETHESDA,MD 20892

[2] NCI,MED BRANCH,BETHESDA,MD 20892

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 03期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/S0960-894X(01)80792-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A structure activity study was conducted on two important members of the styryl class of tyrosine-specific protein kinase inhibitors to examine relative roles which the aryl rings and vinyl side chains play in their inhibitory activity. The ability of four analogs (1a-d) to inhibit autophosphorylation of epidermal growth factor receptor (EGFR) and p56lck tyrosine kinases was examined, with results showing that both the pattern of aromatic hydroxylation and the type of side chain functionality can greatly influence both selectivity and potency.

引用

页码：165 / 168

页数：4

共 25 条

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