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 journalArticle

3 Citations (Scopus)

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)5548-5551
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number18
Early online date18 Jul 2010
DOIs
Publication statusPublished - 15 Sep 2010

Keywords

  • inflammation
  • bone loss
  • rheumatoid arthritis
  • TNFa
  • NFκB
  • RANKL

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