Synthesis and biological evaluation on novel analogs of 9-methylstreptimidone, an inhibitor of NF-kappaB.
Synthesis of 9-methylstreptimidone analogs and their inhibitory activities against NF-kappaB (nuclear factor-kappaB) are reported. Among several active derivatives synthesized in this study, 8 with a relatively simple structure, exhibited inhibitory activity against LPS-induced NO production comparable to that of 9-methylstreptimidone.
Ishikawa
Yuichi
Y
Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.
Tachibana
Miyuki
M
Matsui
Chino
C
Obata
Rika
R
Umezawa
Kazuo
K
Nishiyama
Shigeru
S
D000818:Animals; D000975:Antioxidants / Q000378:metabolism; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D008070:Lipopolysaccharides / Q000737:chemistry*; D051379:Mice; D008956:Models, Chemical; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy*; D009569:Nitric Oxide / Q000737:chemistry*; D010881:Piperidones / Q000138:chemical synthesis* / Q000494:pharmacology*
D000975:Antioxidants; D008070:Lipopolysaccharides; D016328:NF-kappa B; D010881:Piperidones; D009569:Nitric Oxide; C008497:9-methylstreptimidone