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

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 efficacy in vivo to increase the half...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2729-2733
Hauptverfasser:	Mulvihill, Mark J., Kan, Julie L.C., Cooke, Andrew, Bhagwat, Shripad, Beck, Patricia, Bittner, Mark, Cesario, Cara, Keane, David, Lazarescu, Viorica, Nigro, Anthony, Nillson, Christy, Panicker, Bijoy, Smith, Vanessa, Srebernak, Mary, Sun, Feng-Lei, O’Connor, Matthew, Russo, Suzanne, Fischetti, Gia, Vrkljan, Michael, Winski, Shannon, Castelhano, Arlindo L., Emerson, David, Gibson, Neil W.
Format:	Artikel
Sprache:	eng
Schlagworte:	All-trans retinoic acid Antineoplastic agents atRA Biological and medical sciences Cancer Chromatography, High Pressure Liquid CYP26 Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology General aspects Half-Life Mass Spectrometry Medical sciences Naphthalenes - pharmacokinetics Naphthalenes - pharmacology Pharmacology. Drug treatments Propionates - pharmacokinetics Propionates - pharmacology RAMBA Retinoic Acid 4-Hydroxylase Retinoic acid metabolic blocking agents Tretinoin - antagonists & inhibitors Tretinoin - metabolism
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