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

…, C Nillson, B Panicker, V Smith, M Srebernak…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2729 - 2733

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被引用次数: 8

摘要

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.