[Pyridyl-substituted tetralone derivatives: a new class of nonsteroidal aromatase inhibitors]

Arch Pharm (Weinheim). 1991 Oct;324(10):815-20.
[Article in German]

Abstract

Structural modification of flavone and flavanone, two weak inhibitors of aromatase, led to the new compounds 1-7, the syntheses of which are described as well as the evaluation of their aromatase and desmolase inhibitory potency. With the exception of 2 all compounds show a stronger inhibition of aromatase than the parent compounds and are more effective inhibitors than aminoglutethimide (AG), the only commercially available compound. In contrast to AG compounds 1 and 3-7 exhibit no desmolase inhibitory activity. In case of AG this effect leads to undesirable side effects.

Publication types

  • English Abstract

MeSH terms

  • Aromatase Inhibitors*
  • Cholesterol Side-Chain Cleavage Enzyme / antagonists & inhibitors
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Tetrahydronaphthalenes / chemical synthesis*
  • Tetrahydronaphthalenes / pharmacology

Substances

  • Aromatase Inhibitors
  • Pyridines
  • Tetrahydronaphthalenes
  • Cholesterol Side-Chain Cleavage Enzyme