ARYLAMIDES OF HYDROXYLATED ISOQUINOLINES AS PROTEIN-TYROSINE KINASE INHIBITORS

被引：16

作者：

BURKE, TR

FORD, H

OSHEROV, N

LEVITZKI, A

STEFANOVA, I

HORAK, ID

MARQUEZ, VE

机构：

[1] NCI, DIV CANC BIOL DIAG & CTR, METAB BRANCH, BETHESDA, MD 20892 USA

[2] HEBREW UNIV JERUSALEM, DEPT BIOL CHEM, IL-91904 JERUSALEM, ISRAEL

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)80473-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aryl-substituted amides of isomeric 6,7- and 7,8-dihydroxyisoquinoline-3-carboxamides (2 and 3) were prepared. Divergent structural requirements were observed for inhibiting p56lck and epidermal growth factor receptor (EGFR) protein-tyrosine kinases (PTKs), with the 7,8-dihydroxy substitution pattern being essential for p56lck activity, and the arylamide being required for EGFR potency. The work presents a useful approach toward the design of inhibitors which can discriminate between different PTKs.

引用

页码：1771 / 1774

页数：4

共 10 条

[1]

BURKE T R JR, 1992, Drugs of the Future, V17, P119

[2]

BURKE TR, 1992, HETEROCYCLES, V34, P757

[3]

BURKE TR, IN PRESS J MED CHEM

[4]

Dobrusin EM, 1992, ANNU REP MED CHEM, V27, P169