|
|||||
|
|
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors |
|
| Authors: | Gilleron Pauline Wlodarczyk Nicolas Houssin Raymond Farce Amaury Laconde Guillaume Goossens Jean-François Lemoine Amélie Pommery Nicole Hénichart Jean-Pierre Millet Régis |
| Institution: | Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, IFR 114, Université de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille, France. |
| Abstract: | 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 (IC(50)=17.3 nM) and antiproliferative properties. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |