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Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Biggadike, Keith; Caivano, Matilde; Clackers, Margaret; Coe, Diane M; Hardy, George W; Humphreys, Davina; Jones, Haydn T; House, David; Miles-Williams, Annette; Skone, Philip A; Uings, Iain; Weller, Vicki; McLay, Iain M; Macdonald, Simon J F.
Bioorg Med Chem Lett ; 19(16): 4846-50, 2009 Aug 15.
Article in English | MEDLINE | ID: mdl-19592247

ABSTRACT

Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFkappaB agonist activity was optimised in an iterative process from pIC(50) 7.5 (for 7), to pIC(50) 10.1 (for 38E1). An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor.


Subject(s)
Pyrazoles/chemistry , Receptors, Glucocorticoid/agonists , Catalytic Domain , Cell Line , Computer Simulation , Humans , Indazoles/chemistry , NF-kappa B/metabolism , Receptors, Glucocorticoid/metabolism , Structure-Activity Relationship
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