Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists

J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t.

Abstract

We report on the nuclear receptor binding affinities, cellular activities of transrepression and transactivation, and anti-inflammatory properties of a quinol-4-one and other A-ring mimetic containing nonsteroidal class of glucocorticoid agonists.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Aromatase / metabolism
  • Dexamethasone / pharmacology
  • Female
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Glucocorticoids / agonists*
  • HeLa Cells
  • Humans
  • Lipopolysaccharides / pharmacology
  • Mice
  • Mice, Inbred BALB C
  • Molecular Mimicry*
  • Quinolones / chemical synthesis
  • Quinolones / chemistry
  • Quinolones / pharmacology*
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Trans-Activators / chemical synthesis
  • Trans-Activators / chemistry
  • Trans-Activators / pharmacology*
  • Transcriptional Activation

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Glucocorticoids
  • Lipopolysaccharides
  • Quinolones
  • Receptors, Cytoplasmic and Nuclear
  • Trans-Activators
  • Dexamethasone
  • Aromatase