Structure-activity relationships of 6-fluoroquinazolines:: Dual-acting compounds with inhibitory activities toward both TNF-α production and T cell proliferation

被引：30

作者：

Tobe, M ^{[1
]}

Isobe, Y ^{[1
]}

Tomizawa, H ^{[1
]}

Nagasaki, T ^{[1
]}

Obara, F ^{[1
]}

Hayashi, H ^{[1
]}

机构：

[1] Japan Energy Corp, Pharmaceut & Biotechnol Lab, Toda, Saitama 3358502, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0968-0896(02)00338-3

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：

We synthesized various 6-fluoro-7-(1-piperazino)quinazolines based on the structure of I and evaluated their inhibitory activities toward both TNF-alpha production and T cell proliferation responses. Among these compounds, 7a, having the 3,4-(methylenedioxy)phenyl moiety at the C(4)-position of the quinazoline ring, showed both inhibitory activities. Furthermore, the oral treatment with 7a exhibited an anti-inflammatory effect in rats with adjuvant arthritis as well as an inhibitory activity toward LPS-induced TNF-alpha production. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：609 / 616

页数：8

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