title: Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra series.
abstract: Based on the structure of R115777 (tipifarnib, Zarnestra), a series of farnesyltransferase inhibitors have been synthesized by modification of the 2-quinolinone motif and transposition of the 4-chlorophenyl ring to the imidazole or its replacement by 5-membered rings. This has yielded a novel series of potent farnesyltransferase inhibitors.
authors.affiliation: Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development (J&JPRD), Campus de Maigremont BP615, Val de Reuil, France. pangibau@prdfr.jnj.com
authors.forename: Patrick
authors.initials: P
authors.lastname: Angibaud
authors.forename: Laurence
authors.initials: L
authors.lastname: Mevellec
authors.forename: Christophe
authors.initials: C
authors.lastname: Meyer
authors.forename: Xavier
authors.initials: X
authors.lastname: Bourdrez
authors.forename: Patricia
authors.initials: P
authors.lastname: Lezouret
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: Sophie
authors.initials: S
authors.lastname: Merillon
authors.forename: David W
authors.initials: DW
authors.lastname: End
authors.forename: Jacky
authors.initials: J
authors.lastname: Van Dun
authors.forename: Walter
authors.initials: W
authors.lastname: Wouters
authors.forename: Marc
authors.initials: M
authors.lastname: Venet
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015394:Molecular Structure; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D015363:Quinolones; D051231:Farnesyltranstransferase; C402769:tipifarnib