A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5638-42. doi: 10.1016/j.bmcl.2010.08.036. Epub 2010 Aug 11.

Abstract

The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / chemistry*
  • Cell Line, Tumor
  • Cyclohexanones / chemical synthesis
  • Cyclohexanones / chemistry*
  • Cyclohexanones / pharmacology
  • Epoxy Compounds / chemical synthesis
  • Epoxy Compounds / chemistry*
  • Epoxy Compounds / pharmacology
  • Hydroquinones / chemistry*
  • Mice
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism
  • Nitric Oxide / metabolism
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

Substances

  • Benzamides
  • Cyclohexanones
  • Epoxy Compounds
  • Hydroquinones
  • NF-kappa B
  • dehydroxymethylepoxyquinomicin
  • Nitric Oxide