title: 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
abstract: The evaluation of structure-activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.
authors.affiliation: Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research & Development, Campus de Maigremont BP615, 27106 Val de Reuil, France. pangibau@prdfr.jnj.com
authors.forename: Patrick
authors.initials: P
authors.lastname: Angibaud
authors.forename: Xavier
authors.initials: X
authors.lastname: Bourdrez
authors.forename: Ann
authors.initials: A
authors.lastname: Devine
authors.forename: David W
authors.initials: DW
authors.lastname: End
authors.forename: Eddy
authors.initials: E
authors.lastname: Freyne
authors.forename: Yannick
authors.initials: Y
authors.lastname: Ligny
authors.forename: Philippe
authors.initials: P
authors.lastname: Muller
authors.forename: Geert
authors.initials: G
authors.lastname: Mannens
authors.forename: Isabelle
authors.initials: I
authors.lastname: Pilatte
authors.forename: Virginie
authors.initials: V
authors.lastname: Poncelet
authors.forename: Stacy
authors.initials: S
authors.lastname: Skrzat
authors.forename: Gerda
authors.initials: G
authors.lastname: Smets
authors.forename: Jacky
authors.initials: J
authors.lastname: Van Dun
authors.forename: Pieter
authors.initials: P
authors.lastname: Van Remoortere
authors.forename: Marc
authors.initials: M
authors.lastname: Venet
authors.forename: Walter
authors.initials: W
authors.lastname: Wouters
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051231:Farnesyltranstransferase; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D051379:Mice; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D001381:Azepines; D007202:Indicators and Reagents; D011799:Quinazolines; D015363:Quinolones; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C402769:tipifarnib