Advances Toward Dissociated Non-Steroidal Glucocorticoid Receptor Agonists

摘要: Publisher Summary This chapter discusses dissociated non-steroidal glucocorticoid receptor agonists such as fluorocortivazol analogs, hydroxy-trifluoromethyl-phenyl-pentanoic (HTPP) aryl amides (HTPP D-rings and HTPP A-rings), dihydro-1H-benzopyrano‘3,4-f ]quinolines (DBQ), ring-opened DBQ additional fused cyclic cores, sulfonamide-linked scaffolds. The C- of the steroidal (GR) agonist can be substantially modified without losing activity. Other D-ring analogs were systematically evaluated for transcriptional activation (TA) receptors (TR) in osteosarcoma cells. disclosure (+)-enantiomer spurred extensive structure–activity relationship (SAR) scaffold modifications to 2-hydroxy-2-trifluoromethyl-4-methyl-4-phenyl-pentanoic scaffold. (DBQ) used hormone ligands. A series are reported. For example, 6-phenyldihydroquinoline derivatives containing a phenethyl thioether at C-4 bind selectively GR exhibit only antagonist Fused include dibenzodiazepines dibenzoazepines. Sulfonamide-linked a- methyltryptamines originally identified modulators during HTS campaign. Subsequent structural led increases binding agonistic