Identification of tertiary sulfonamides as RORc inverse agonists

Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Herein, we describe the identification of compounds with improved RORc biochemical inverse agonist activity and cellular potencies. These improved compounds also possessed a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (9), p.2182-2187
Hauptverfasser:	Fauber, Benjamin P., René, Olivier, Burton, Brenda, Everett, Christine, Gobbi, Alberto, Hawkins, Julie, Johnson, Adam R., Liimatta, Marya, Lockey, Peter, Norman, Maxine, Wong, Harvey
Format:	Artikel
Sprache:	eng
Schlagworte:	Autoimmune Humans IL-17 Inflammation Ligands Molecular Docking Simulation Nuclear Receptor Subfamily 1, Group F, Member 3 - agonists Nuclear Receptor Subfamily 1, Group F, Member 3 - metabolism RORc RORγ Structure-Activity Relationship Sulfonamides - chemistry Sulfonamides - pharmacology
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