1.
Bioorg Med Chem Lett
; 21(4): 1126-33, 2011 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21257309
RESUMO
A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides which interact with the extended ligand binding domain. This series has produced some of the most potent and least lipophilic agonists of which we are aware such as 20a (NFκB pIC(50) 8.3 (100%), clogP 1.9). Certain analogues in this series also display evidence for modulated pharmacology.