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Discovery of biphenylketones as dual modulators of inflammation and bone loss

  作者 Greig, IR; Coste, E; Ralston, SH; van't Hof, RJ  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2010年20-18;  页码  5548-5551  
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[摘要]Biphenylketones were identified as novel inhibitors of NF kappa B activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 mu M), showed oral activity, and was able to completely prevent inflammation and bone loss in vivo. (C) 2010 Elsevier Ltd. All rights reserved.

 
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