Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist

Org Biomol Chem. 2013 Sep 21;11(35):5782-6. doi: 10.1039/c3ob41264d.

Abstract

Total synthesis of eryvarin H and a biological investigation of its analogues as a potential inverse agonist of ERRγ are described here. Among the 13 analogues prepared by the modular synthetic route, eryvarin H and compound showed meaningful ERRγ inverse agonistic activities along with moderate selectivity over ERα and other nuclear receptors in the cell-based reporter gene assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chromones / chemical synthesis*
  • Chromones / pharmacology*
  • Erythrina / chemistry*
  • Estrogen Receptor alpha / agonists
  • Estrogen Receptor alpha / metabolism
  • HEK293 Cells
  • Humans
  • Models, Molecular
  • Molecular Docking Simulation
  • Receptors, Estrogen / agonists*
  • Receptors, Estrogen / metabolism

Substances

  • Chromones
  • Estrogen Receptor alpha
  • Receptors, Estrogen
  • eryvarin H
  • estrogen receptor gamma