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Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Clackers, Margaret; Coe, Diane M; Demaine, Derek A; Hardy, George W; Humphreys, Davina; Inglis, Graham G A; Johnston, Michael J; Jones, Haydn T; House, David; Loiseau, Richard; Minick, Doug J; Skone, Philip A; Uings, Iain; McLay, Iain M; Macdonald, Simon J F.
Afiliación
  • Clackers M; Medicines Research Centre, riCEDD, GlaxoSmithKline, Stevenage, UK.
Bioorg Med Chem Lett ; 17(17): 4737-45, 2007 Sep 01.
Article en En | MEDLINE | ID: mdl-17616395
Starting from an established series of non-steroidal glucocorticoid receptor (GR) agonists, a large array was designed where a metabolically labile benzoxazinone moiety was replaced. Initial hits bound to GR but lacked agonist activity. Following two further iterations, potent GR agonists were discovered with 20D1E1 having NFkappaB agonism pIC(50) 8.8 (103%). Other analogues such as 23D1E1 display a dissociated profile (NFkappaB pIC(50) 8.1 (103%), MMTV pEC(50) 7.02 (36%)). The tetrahydronaphthalene moiety can also be replaced with substituted aryls such as 24E1 and 25E1.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Receptores de Glucocorticoides / Glucocorticoides Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article Pais de publicación: Reino Unido
Buscar en Google
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Receptores de Glucocorticoides / Glucocorticoides Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article Pais de publicación: Reino Unido