875796-66-0Relevant academic research and scientific papers
Nonsteroidal glucocorticoid agonists: Tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (Transrepression/Transactivation) efficacy selectivity
Biggadike, Keith,Boudjelal, Mohamed,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,Needham, Deborah,Skone, Philip A.,Uings, Iain,Veitch, Gemma,Weingarten, Gordon G.,McLay, Iain M.,Macdonald, Simon J. F.
, p. 6519 - 6534 (2008/09/17)
The synthesis and biological activity of tetrahydronaphthalene derivatives coupled to various heterocycles are described. These compounds are potent glucocorticoid receptor agonists with efficacy selectivity in an NFκB glucocorticoid receptor (GR) agonist assay (representing transrepression effects) over an MMTV GR agonist assay (representing transactivation effects). Quinolones, indoles, and C- and N-linked quinolines are some of the heterocycles that provide efficacy selectivity. For example, the isoquinoline 49D1E2 has NFκB agonism with pIC50 of 8.66 (89%) and reduced efficacy in MMTV agonism (6%), and the quinoline 55D1E1 has NFκB agonism with pIC 50 of 9.30 (101%) and reduced efficacy in MMTV agonism with pEC 50 of 8.02 (47%). A description of how a compound from each class is modeled in the active site of the receptor is given.
TETRAHYDRO-NAPHTHALENE DERIVATIVES AS GLUCOCORTICOID RECEPTOR MODULATORS
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Page/Page column 36, (2010/10/19)
The present invention is directed to compounds of formula (I): wherein R represents a methyl or an ethyl group X represents N, C-H or C-CH3 when X represents C-H or C-CH3, Y represents N when X represents N, Y represents C-H and phys
