Identification of tertiary sulfonamides as RORc inverse agonists.

Bioorganic & Medicinal Chemistry Letters(2014)

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摘要
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.
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关键词
RORc,RORγ,IL-17,Inflammation,Autoimmune
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