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 language | English |
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Pages (from-to) | 5548-5551 |
Number of pages | 4 |
Journal | Bioorganic & Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 18 |
Early online date | 18 Jul 2010 |
DOIs | |
Publication status | Published - 15 Sept 2010 |
Keywords
- inflammation
- bone loss
- rheumatoid arthritis
- TNFa
- NFκB
- RANKL
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