Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists

  • Fauber B
  • Gobbi A
  • Savy P
 et al. 
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A high-throughput screen of the Genentech/Roche compound collection using a retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) biochemical assay revealed a N-sulfonyl-tetrahydroquinoline hit. Herein, we describe the hit-to-lead optimization and structure-activity relationships of these tetrahydroquinoline RORc inverse agonists. Through iterative synthesis and analog design, we identified compounds with improved biochemical RORc inverse agonist activity and RORc cellular potencies. These improved N-sulfonyl-tetrahydroquinoline compounds also exhibited selectivity for RORc over other nuclear receptors.

Author-supplied keywords

  • Autoimmune
  • IL-17
  • Inflammation
  • RORc
  • RORγ

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  • Benjamin P. Fauber

  • Alberto Gobbi

  • Pascal Savy

  • Brenda Burton

  • Yuzhong Deng

  • Christine Everett

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