Discovery of Novel Benzopyranyl Tetracycles that Act as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-kappa B Ligand

Title
Discovery of Novel Benzopyranyl Tetracycles that Act as Inhibitors of Osteoclastogenesis Induced by Receptor Activator of NF-kappa B Ligand
Authors
이상희주명언김명희배수정김성환박승범
Issue Date
2010-12
Publisher
Journal of medicinal chemistry
Citation
VOL 53, NO 24-8764
Abstract
A novel benzopyran-fused molecular framework 7ai was discovered as a specific inhibitor of RANKL-induced osteoclastogenesis using a cell-based TRAP activity assay from drug-like small-molecule libraries constructed by diversity-oriented synthesis. Its inhibitory activity was confirmed by in vitro evaluations including specific inhibition of RANKL-induced ERK phosphorylation and NF-kappa B transcriptional activation. 7ai can serve as a specific small-molecule modulator for mechanistic studies of RANKL-induced osteoclast differentiation as well as a potential lead for the development of antiresorptive drugs.
URI
http://pubs.kist.re.kr/handle/201004/67186
ISSN
0022-2623
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KIST Publication > Article
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