Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) …
K Biggadike, M Boudjelal, M Clackers…
文献索引：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. Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6519 - 6534
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 ...
