Design and synthesis of a new type of non steroidal human aromatase inhibitors

Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4. doi: 10.1016/s0960-894x(98)00157-7.

Abstract

The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1 (MR20814), allowed us to design some related derivatives as potential new inhibitors. Among those we synthesized, chlorophenylpyridylmethylenetetrahydroindolizinone 5 (MR20492) exhibited in vitro a ten-fold higher inhibition of the enzyme (IC50 = 0.2 +/- 0.0 microM and Ki = 10.3 +/- 3.3 nM).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aromatase Inhibitors*
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Fadrozole / chemistry
  • Fadrozole / pharmacology
  • Female
  • Humans
  • Indicators and Reagents
  • Indolizines / chemical synthesis*
  • Indolizines / chemistry
  • Indolizines / pharmacology
  • Microsomes / enzymology
  • Placenta / enzymology
  • Pregnancy
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Structure-Activity Relationship
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Aromatase Inhibitors
  • Enzyme Inhibitors
  • Indicators and Reagents
  • Indolizines
  • MR 20492
  • Pyridines
  • Triazoles
  • vorozole
  • Fadrozole