title: Potent, non-thiol inhibitors of farnesyltransferase.
abstract: The structure-activity relationship of a series of non-thiol CaaX analogs, which are inhibitors of farnesyltransferase, is described. These inhibitors contain a substituted phenyl group at the N terminus, which may occupy a novel binding domain on the Ras protein.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
authors.forename: M J
authors.initials: MJ
authors.lastname: Breslin
authors.forename: S J
authors.initials: SJ
authors.lastname: deSolms
authors.forename: E A
authors.initials: EA
authors.lastname: Giuliani
authors.forename: G E
authors.initials: GE
authors.lastname: Stokker
authors.forename: S L
authors.initials: SL
authors.lastname: Graham
authors.forename: D L
authors.initials: DL
authors.lastname: Pompliano
authors.forename: S D
authors.initials: SD
authors.lastname: Mosser
authors.forename: K A
authors.initials: KA
authors.lastname: Hamilton
authors.forename: J H
authors.initials: JH
authors.lastname: Hutchinson
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase