Discovery of biphenylketones as dual modulators of inflammation and bone loss

Iain R Greig, Emmanuel Coste, Stuart H Ralston, Rob J van't Hof

Research output: Contribution to journalArticlepeer-review

Abstract

Biphenylketones were identified as novel inhibitors of NFkappaB activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50=0.8 microM), showed oral activity, and was able to completely prevent inflammation and bone loss in vivo.
Original languageEnglish
Pages (from-to)5548-51
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number18
DOIs
Publication statusPublished - 2010

Keywords

  • Animals
  • Anti-Inflammatory Agents
  • Arthritis
  • Benzene Derivatives
  • Cell Line
  • Cell Survival
  • Female
  • Inflammation
  • Ketones
  • Macrophages
  • Mice
  • NF-kappa B
  • Osteoclasts
  • Osteoporosis
  • Polycyclic Hydrocarbons, Aromatic
  • Structure-Activity Relationship
  • Tumor Necrosis Factor-alpha

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