Discovery of biphenylketones as dual modulators of inflammation and bone loss

Iain R Greig; Emmanuel Coste; Stuart H Ralston; Rob J van't Hof

doi:10.1016/j.bmcl.2010.07.055

Discovery of biphenylketones as dual modulators of inflammation and bone loss

Iain R Greig, Emmanuel Coste, Stuart H Ralston, Rob J van't Hof

Medical Sciences

Research output: Contribution to journal › Article › peer-review

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 language	English
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	https://doi.org/10.1016/j.bmcl.2010.07.055
Publication status	Published - 15 Sept 2010

Keywords

inflammation
bone loss
rheumatoid arthritis
TNFa
NFκB
RANKL

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10.1016/j.bmcl.2010.07.055

Discovery and commercialisation of new drug for rheumatoid arthritis and related conditions
Iain Greig (Coordinator), Stuart Ralston (Coordinator) & Rob. J. van't Hof (Coordinator)
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title = "Discovery of biphenylketones as dual modulators of inflammation and bone loss",

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.",

keywords = "inflammation, bone loss, rheumatoid arthritis, TNFa, NFκB, RANKL",

author = "Greig, {Iain R} and Emmanuel Coste and Ralston, {Stuart H} and {van't Hof}, {Rob J}",

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AU - Greig, Iain R

AU - Coste, Emmanuel

AU - Ralston, Stuart H

AU - van't Hof, Rob J

PY - 2010/9/15

Y1 - 2010/9/15

N2 - 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.

AB - 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.

KW - inflammation

KW - bone loss

KW - rheumatoid arthritis

KW - TNFa

KW - NFκB

KW - RANKL

U2 - 10.1016/j.bmcl.2010.07.055

DO - 10.1016/j.bmcl.2010.07.055

M3 - Article

C2 - 20692834

SN - 0960-894X

VL - 20

SP - 5548

EP - 5551

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 18

ER -

Discovery of biphenylketones as dual modulators of inflammation and bone loss

Abstract

Keywords

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Impacts

Discovery and commercialisation of new drug for rheumatoid arthritis and related conditions

Cite this