title: 3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent.
abstract: 3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid and analogs were designed and synthesized as highly potent and selective CYP26 inhibitors, serving as retinoic acid metabolic blocking agents (RAMBAs), with demonstrated in vivo efficacy to increase the half-life of exogenous atRA.
authors.affiliation: OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. mmulvihill@osip.com
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Mulvihill
authors.forename: Julie L C
authors.initials: JL
authors.lastname: Kan
authors.forename: Andrew
authors.initials: A
authors.lastname: Cooke
authors.forename: Shripad
authors.initials: S
authors.lastname: Bhagwat
authors.forename: Patricia
authors.initials: P
authors.lastname: Beck
authors.forename: Mark
authors.initials: M
authors.lastname: Bittner
authors.forename: Cara
authors.initials: C
authors.lastname: Cesario
authors.forename: David
authors.initials: D
authors.lastname: Keane
authors.forename: Viorica
authors.initials: V
authors.lastname: Lazarescu
authors.forename: Anthony
authors.initials: A
authors.lastname: Nigro
authors.forename: Christy
authors.initials: C
authors.lastname: Nillson
authors.forename: Bijoy
authors.initials: B
authors.lastname: Panicker
authors.forename: Vanessa
authors.initials: V
authors.lastname: Smith
authors.forename: Mary
authors.initials: M
authors.lastname: Srebernak
authors.forename: Feng-Lei
authors.initials: FL
authors.lastname: Sun
authors.forename: Matthew
authors.initials: M
authors.lastname: O'Connor
authors.forename: Suzanne
authors.initials: S
authors.lastname: Russo
authors.forename: Gia
authors.initials: G
authors.lastname: Fischetti
authors.forename: Michael
authors.initials: M
authors.lastname: Vrkljan
authors.forename: Shannon
authors.initials: S
authors.lastname: Winski
authors.forename: Arlindo L
authors.initials: AL
authors.lastname: Castelhano
authors.forename: David
authors.initials: D
authors.lastname: Emerson
authors.forename: Neil W
authors.initials: NW
authors.lastname: Gibson
mesh_terms: D002851:Chromatography, High Pressure Liquid; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D006207:Half-Life; D013058:Mass Spectrometry; D009281:Naphthalenes / Q000493:pharmacokinetics / Q000494:pharmacology*; D011422:Propionates / Q000493:pharmacokinetics / Q000494:pharmacology*; D000072516:Retinoic Acid 4-Hydroxylase; D014212:Tretinoin / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: C512307:3-(6-(2-dimethylamino-1-imidazol-1-yl-butyl)naphthalen-2-yloxy)-2,2-dimethyl-propionic acid; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D009281:Naphthalenes; D011422:Propionates; D014212:Tretinoin; D003577:Cytochrome P-450 Enzyme System; D000072516:Retinoic Acid 4-Hydroxylase