New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation

Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. doi: 10.1016/j.bmc.2007.10.057. Epub 2007 Oct 22.


Some natural compounds such as flavonoids are known to possess a moderate inhibitory activity against aromatase, this enzyme being an interesting target for hormone-dependent breast cancer treatment. It has been demonstrated that the modulation of flavonoid skeleton could increase anti-aromatase effect. Therefore, new 7,8-benzoflavanones were synthesized and tested for their activity toward aromatase inhibition. It was observed that the introduction of a benzo ring at position C-7 and C-8 on flavanone skeleton led to new potent aromatase inhibitors, the resulting 7,8-benzoflavanones being until nine times more potent than aminogluthetimide (the first aromatase inhibitor used clinically).

MeSH terms

  • Anastrozole
  • Aromatase Inhibitors / chemical synthesis*
  • Aromatase Inhibitors / chemistry
  • Aromatase Inhibitors / pharmacology*
  • Benzene / chemistry*
  • Cyclization
  • Flavanones / chemical synthesis*
  • Flavanones / chemistry
  • Flavanones / pharmacology*
  • Humans
  • Hydrogen Bonding
  • Letrozole
  • Microsomes / drug effects
  • Microsomes / enzymology
  • Molecular Structure
  • Nitriles / chemistry
  • Structure-Activity Relationship
  • Triazoles / chemistry


  • Aromatase Inhibitors
  • Flavanones
  • Nitriles
  • Triazoles
  • Anastrozole
  • Letrozole
  • Benzene
  • flavanone