Author/Authors :
Jie-Fei Cheng، نويسنده , , Chin-Mi Chen، نويسنده , , David Wallace، نويسنده , , Sovouthy Tith، نويسنده , , Thomas Arrhenius، نويسنده , , Hirotaka Kashiwagi، نويسنده , , Yoshiyuki Ono، نويسنده , , Akira Ishikawa, Terry L. Wilson، نويسنده , , Haruhiko Sato، نويسنده , , Toshiro Kozono، نويسنده , , Hediki Sato، نويسنده , , Alex M. Nadzan، نويسنده ,
Abstract :
The discovery and structure–activity relationship of a novel series of coumarin-based TNF-α 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-α production by human peripheral blood mononuclear cells (hPBMC), stimulated by bacterial lipopolysaccharide (LPS). Selected compounds also demonstrated in vivo inhibition of TNF-α production in rats.
Keywords :
TNF-a.* Corresponding author at present address: Tanabe Research LaboratoriesUSA , 4540 Towne Centre Court , CA 92121 , USA. Tel.: +1-858-622-7029 , e-mail: jcheng@trlusa.com , Coumarin , fax: +1-858-538-9383 , San Diego , Inc.
