Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) …

K Biggadike, M Boudjelal, M Clackers…

Index: 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

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Citation Number: 37

Abstract

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 ...