| Literature DB >> 15109623 |
Jie-Fei Cheng1, Mi Chen, David Wallace, Sovouthy Tith, Thomas Arrhenius, Hirotaka Kashiwagi, Yoshiyuki Ono, Akira Ishikawa, Haruhiko Sato, Toshiro Kozono, Hediki Sato, Alex M Nadzan.
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.Entities:
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Year: 2004 PMID： 15109623 DOI： 10.1016/j.bmcl.2004.03.022
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823