title: Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.
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.
authors.affiliation: Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, IFR 114, Université de Lille 2, 3 rue du Professeur Laguesse, BP 83, 59006 Lille, France.
authors.forename: Pauline
authors.initials: P
authors.lastname: Gilleron
authors.forename: Nicolas
authors.initials: N
authors.lastname: Wlodarczyk
authors.forename: Raymond
authors.initials: R
authors.lastname: Houssin
authors.forename: Amaury
authors.initials: A
authors.lastname: Farce
authors.forename: Guillaume
authors.initials: G
authors.lastname: Laconde
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Goossens
authors.forename: Amélie
authors.initials: A
authors.lastname: Lemoine
authors.forename: Nicole
authors.initials: N
authors.lastname: Pommery
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Hénichart
authors.forename: Régis
authors.initials: R
authors.lastname: Millet
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors*; D006801:Humans; D007939:Leukemia L1210; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles