Synthesis and biological evaluation on novel analogs of 9-methylstreptimidone, an inhibitor of NF-kappaB

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1726-8. doi: 10.1016/j.bmcl.2009.01.107. Epub 2009 Feb 5.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / metabolism
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Jurkat Cells
  • Lipopolysaccharides / chemistry*
  • Mice
  • Models, Chemical
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / chemistry
  • Neoplasms / drug therapy*
  • Nitric Oxide / chemistry*
  • Piperidones / chemical synthesis*
  • Piperidones / pharmacology*

Substances

  • Antioxidants
  • Lipopolysaccharides
  • NF-kappa B
  • Piperidones
  • Nitric Oxide
  • 9-methylstreptimidone