title: Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
abstract: A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition.
authors.affiliation: Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&JPRD), 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: David W
authors.initials: DW
authors.lastname: End
authors.forename: Eddy
authors.initials: E
authors.lastname: Freyne
authors.forename: Michel
authors.initials: M
authors.lastname: Janicot
authors.forename: Patricia
authors.initials: P
authors.lastname: Lezouret
authors.forename: Yannick
authors.initials: Y
authors.lastname: Ligny
authors.forename: Geert
authors.initials: G
authors.lastname: Mannens
authors.forename: Siegrid
authors.initials: S
authors.lastname: Damsch
authors.forename: Laurence
authors.initials: L
authors.lastname: Mevellec
authors.forename: Christophe
authors.initials: C
authors.lastname: Meyer
authors.forename: Philippe
authors.initials: P
authors.lastname: Muller
authors.forename: Isabelle
authors.initials: I
authors.lastname: Pilatte
authors.forename: Virginie
authors.initials: V
authors.lastname: Poncelet
authors.forename: Bruno
authors.initials: B
authors.lastname: Roux
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; D002455:Cell Division / Q000187:drug effects; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D051231:Farnesyltranstransferase; D007700:Kinetics; D008968:Molecular Conformation; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011799:Quinazolines; D011804:Quinolines; D015363:Quinolones; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C402769:tipifarnib