Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1549-52. doi: 10.1016/j.bmcl.2005.12.043. Epub 2005 Dec 28.

Abstract

We report the discovery of a novel class of glucocorticoid receptor (GR) ligands based on 1,2-dihydroquinoline molecular scaffold. The compounds exhibit good GR binding affinity and selectivity profile against other nuclear hormone receptors.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Inflammatory Agents / pharmacology
  • Dexamethasone / pharmacology
  • HeLa Cells
  • Humans
  • Interleukin-1 / pharmacology
  • Interleukin-6 / metabolism
  • Ligands
  • Mammary Tumor Virus, Mouse / genetics
  • Models, Molecular
  • Molecular Structure
  • Promoter Regions, Genetic / drug effects
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Receptors, Estrogen / drug effects
  • Receptors, Estrogen / metabolism
  • Receptors, Glucocorticoid / antagonists & inhibitors*
  • Receptors, Glucocorticoid / metabolism*
  • Receptors, Mineralocorticoid / drug effects
  • Receptors, Mineralocorticoid / metabolism
  • Receptors, Progesterone / drug effects
  • Receptors, Progesterone / metabolism
  • Structure-Activity Relationship
  • Transcription, Genetic / drug effects
  • Transcriptional Activation / drug effects
  • Transcriptional Activation / genetics

Substances

  • Anti-Inflammatory Agents
  • Interleukin-1
  • Interleukin-6
  • Ligands
  • Quinolines
  • Receptors, Estrogen
  • Receptors, Glucocorticoid
  • Receptors, Mineralocorticoid
  • Receptors, Progesterone
  • Dexamethasone