Benzobicyclooctanes as novel inhibitors of TNF-alpha signaling

Bioorganic & Medicinal Chemistry Letters
Randy W JacksonIhab S Darwish

Abstract

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.

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Citations

Jul 2, 2003·Expert Opinion on Investigational Drugs·W I de Boer
Jan 1, 2012·Journal of the American Statistical Association·Yanyuan Ma, Liping Zhu
Dec 17, 2020·International Journal of Molecular Sciences·Nasir JavaidSangdun Choi
Nov 15, 2005·Science·Molly M HeBrian C Cunningham

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis