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Discovery of biphenylketones as dual modulators of inflammation and bone loss
Iain R Greig1, Emmanuel Coste, Stuart H Ralston
1School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen AB25 2ZD, United Kingdom. i.greig@abdn.ac.uk
Bioorganic & Medicinal Chemistry Letters
|August 10, 2010
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.