title: Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors.
abstract: Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC(50) values of 0.7 and 0.6 μM, respectively.
authors.affiliation: Department of Organic Chemistry, Al. I. Cuza University of Iasi, Faculty of Chemistry, Bd. Carol I nr. 11, 700506 Iasi, Romania.
authors.forename: Cristina-Maria
authors.initials: CM
authors.lastname: Abuhaie
authors.forename: Alina
authors.initials: A
authors.lastname: Ghinet
authors.forename: Amaury
authors.initials: A
authors.lastname: Farce
authors.forename: Joëlle
authors.initials: J
authors.lastname: Dubois
authors.forename: Philippe
authors.initials: P
authors.lastname: Gautret
authors.forename: Benoît
authors.initials: B
authors.lastname: Rigo
authors.forename: Dalila
authors.initials: D
authors.lastname: Belei
authors.forename: Elena
authors.initials: E
authors.lastname: Bîcu
mesh_terms: D020134:Catalytic Domain; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D010640:Phenothiazines / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D010640:Phenothiazines; D051231:Farnesyltranstransferase