Discovery of biphenylketones as dual modulators of inflammation and bone loss

IR Greig, E Coste, SH Ralston, RJ van't Hof

Index: Greig, Iain R.; Coste, Emmanuel; Ralston, Stuart H.; Van'T Hof, Rob J. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 18 p. 5548 - 5551

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Abstract

Biphenylketones were identified as novel inhibitors of NFκB activation. Structure–activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50= 0.8 μM), showed oral activity, and was able to completely prevent inflammation and bone loss in vivo.