Novel chromene derivatives as TNF-alpha inhibitors.
A novel series of chromene-based TNF-alpha inhibitors is described. These chromene derivatives inhibit bacterial lipopolysaccharide (LPS) stimulated production of TNF-alpha from human peripheral blood mononuclear cells (PBMC). Additionally, these compounds inhibit NF-kB mediated transcription activation.
Cheng
Jie-Fei
JF
Department of Chemistry, Chugai Pharma USA, 6275 Nancy Ridge Drive, San Diego, CA 92121, USA. jcheng@chungai-pharm.com
Ishikawa
Akira
A
Ono
Yoshinori
Y
Arrhenius
Thomas
T
Nadzan
Alex
A
D001578:Benzopyrans / Q000494:pharmacology*; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D007202:Indicators and Reagents; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D016328:NF-kappa B / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D015533:Transcriptional Activation / Q000187:drug effects; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*
D001578:Benzopyrans; D007202:Indicators and Reagents; D008070:Lipopolysaccharides; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha