Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols')

被引：115
作者：
Lion, Cedric J.
Matthews, Charles S.
Wells, Geoffrey
Bradshaw, Tracey D.
Stevens, Malcolm F. G.
Westwell, Andrew D. [1 ]
机构：
[1] Univ Nottingham, Sch Pharm, Ctr Biomol Sci, Nottingham NG7 2RD, England
[2] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, Wales
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 19期
关键词：
antitumour agents; fluorinated benzothiazoles; thioredoxin;
D O I：
10.1016/j.bmcl.2006.07.072
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and in vitro antitumour evaluation of a new series of fluorinated benzothiazole-substituted 4-hydroxycyclohexa-2,5-dienones ('quinols') is described. The new compounds were found to be of comparable activity compared to the nonfluorinated precursor PMX 464, in terms of antiproliferative activity in sensitive human cancer cell lines (nanomolar GI(50) values) and inhibitory activity against the thioredoxin signalling system. (c) 2006 Elsevier Ltd. All rights reserved.
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收藏
页码：5005 / 5008
页数：4
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