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.

作者信息

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

机构信息

OSI Pharmaceuticals, Inc., 1 Bioscience Park Drive, Farmingdale, NY 11735, USA.

出版信息

Bioorg Med Chem Lett. 2006 May 15;16(10):2729-33. doi: 10.1016/j.bmcl.2006.02.020. Epub 2006 Feb 28.

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.