Benzobicyclooctanes as novel inhibitors of TNF-α signaling

A novel series of TNF-alpha inhibitors based on a benzobicyclooctane scaffold is reported. The compounds display good potency in inhibiting TNF-alpha induced apoptosis and NF kappa B activation. Additionally, they are selective for TNF-alpha as they do not inhibit apoptosis induced by soluble Fas li...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-04, Vol.12 (7), p.1093-1097
Hauptverfasser:	JACKSON, Randy W, GELINAS, Richard, BAUGHMAN, Ted A, COX, Thomas, HOWBERT, J. Jeffry, KUCERA, Kristin A, LATHAM, John A, RAMSDELL, Fred, SINGH, Devinder, DARWISH, Ihab S
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis - drug effects Apoptosis - physiology Biological and medical sciences Fas Ligand Protein Humans Immunomodulators Lung Neoplasms - drug therapy Medical sciences Membrane Glycoproteins - pharmacology Molecular Structure NF-kappa B - drug effects NF-kappa B - metabolism Octanes - pharmacology Pharmacology. Drug treatments Signal Transduction - physiology Tumor Cells, Cultured - drug effects Tumor Necrosis Factor-alpha - antagonists & inhibitors Tumor Necrosis Factor-alpha - metabolism Tumor Necrosis Factor-alpha - pharmacology
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Zusammenfassung:	A novel series of TNF-alpha inhibitors based on a benzobicyclooctane scaffold is reported. The compounds display good potency in inhibiting TNF-alpha induced apoptosis and NF kappa B activation. Additionally, they are selective for TNF-alpha as they do not inhibit apoptosis induced by soluble Fas ligand. The compounds described here can act as leads for future medicinal chemistry efforts and may also be useful tools for elucidating the TNF-alpha signaling pathway.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00098-7