Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2004 May 17;14(10):2411-5.
doi: 10.1016/j.bmcl.2004.03.022.

Discovery and structure-activity relationship of coumarin derivatives as TNF-alpha inhibitors

Jie-Fei Cheng  1 , Mi Chen, David Wallace, Sovouthy Tith, Thomas Arrhenius, Hirotaka Kashiwagi, Yoshiyuki Ono, Akira Ishikawa, Haruhiko Sato, Toshiro Kozono, Hediki Sato, Alex M Nadzan
Affiliations

Discovery and structure-activity relationship of coumarin derivatives as TNF-alpha inhibitors

Jie-Fei Cheng et al. Bioorg Med Chem Lett. .

Abstract

The discovery and structure-activity relationship of a novel series of coumarin-based TNF-alpha inhibitors is described. Starting from the initial lead 1a, various derivatives were prepared surrounding the coumarin core structure to optimize the in vitro inhibitory activity of TNF-alpha production by human peripheral blood mononuclear cells (hPBMC), stimulated by bacterial lipopolysaccharide (LPS). Selected compounds also demonstrated in vivo inhibition of TNF-alpha production in rats.

PubMed Disclaimer

MeSH terms

LinkOut - more resources