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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 |
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| Authors: | 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 |
| Institution: | OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. mmulvihill@osip.com |
| 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. |
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