1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2105-8. doi: 10.1016/s0960-894x(99)00328-5.

Abstract

The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles is described. The compounds were tested for human placental aromatase inhibition in vitro, using [1beta-3H]-androstenedione as the substrate for the aromatase enzyme, the percentage inhibition and IC50 data is included.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoglutethimide / pharmacology
  • Androstenedione / metabolism
  • Aromatase / metabolism
  • Aromatase Inhibitors*
  • Benzofurans / chemistry
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Female
  • Humans
  • Inhibitory Concentration 50
  • Ketones / chemical synthesis
  • Placenta / enzymology
  • Pregnancy
  • Structure-Activity Relationship
  • Tetrazoles / chemistry*
  • Triazoles / chemistry*

Substances

  • Aromatase Inhibitors
  • Benzofurans
  • Enzyme Inhibitors
  • Ketones
  • Tetrazoles
  • Triazoles
  • Aminoglutethimide
  • Androstenedione
  • Aromatase