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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.