Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors

被引：38
作者：
Gilleron, Pauline
Wlodarczyk, Nicolas
Houssin, Raymond
Farce, Amaury
Laconde, Guillaume
Goossens, Jean-Francois
Lemoine, Amelie
Pommery, Nicole
Henichart, Jean-Pierre
Millet, Regis
机构：
[1] Univ Lille 2, Inst Chim Pharmaceut Albert Lespagnol, IFR 114, F-59006 Lille, France
[2] Univ Lille 2, Chim Therapeut Lab, Fac Sci Pharmaceut & Biol, F-59006 Lille, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 19期
关键词：
farnesyltransferase; cytotoxicity; cancer; dioxodibenzothiazepine; dibenzocycloheptane;
D O I：
10.1016/j.bmcl.2007.07.002
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of FTase inhibitors containing a tricyclic moiety-dioxodibenzothiazepine or dibenzocycloheptane-has been designed and synthesized. Among them, dioxodibenzothiazepine 18d displayed significant inhibitory FTase activity (IC50 = 17.3 nM) and antiproliferative properties. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5465 / 5471
页数：7
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