title: Synthesis and evaluation of a novel series of farnesyl protein transferase inhibitors as non-peptidic CAAX tetrapeptide analogues.
abstract: A novel series of compounds, derived from 4-amino-phenyl piperazine, has been designed to selectively inhibit farnesyl protein transferase (FPTase) as CAAX tetrapeptide analogues. Certain of these compounds were shown to possess low nanomolar inhibitory activity both against the isolated enzyme and in cultured cells.
authors.affiliation: Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin, 81106 Cedex, Castres, France. michel.perez@pierre-fabre.com
authors.forename: Michel
authors.initials: M
authors.lastname: Perez
authors.forename: Catherine
authors.initials: C
authors.lastname: Maraval
authors.forename: Stephan
authors.initials: S
authors.lastname: Dumond
authors.forename: Marie
authors.initials: M
authors.lastname: Lamothe
authors.forename: Philippe
authors.initials: P
authors.lastname: Schambel
authors.forename: Chantal
authors.initials: C
authors.lastname: Etiévant
authors.forename: Bridget
authors.initials: B
authors.lastname: Hill
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008565:Membrane Proteins / Q000737:chemistry; D008958:Models, Molecular; D009842:Oligopeptides / Q000737:chemistry; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017368:Protein Prenylation / Q000187:drug effects; D013329:Structure-Activity Relationship; D014166:Transferases / Q000037:antagonists & inhibitors; D014407:Tumor Cells, Cultured; D018631:ras Proteins / Q000187:drug effects / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D008565:Membrane Proteins; D009842:Oligopeptides; D010879:Piperazines; C109563:RTL8C protein, human; D014166:Transferases; D019883:Alkyl and Aryl Transferases; C083291:geranylgeranyltransferase type-I; C064911:p21(ras) farnesyl-protein transferase; D018631:ras Proteins