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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Zusammenfassung:	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 appreciable selectivity for RORc over other nuclear receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.03.038