Diaryl naphthyl methanes a novel class of anti-implantation agents

Bioorg Med Chem. 2004 Mar 1;12(5):1011-21. doi: 10.1016/j.bmc.2003.12.015.

Abstract

Diaryl naphthyl methanes and the corresponding 1, 2, 3, 4- and 5, 6, 7, 8-tetrahydro naphthyl methane derivatives have been synthesized as novel estrogen receptor binding ligands. The secondary and tertiary amino alkoxy derivatives of diaryl naphthyl and tetrahydro naphthyl methane interact with the estrogen receptor to elicit promising estrogenic, antiestrogenic and implantation inhibition activities in rats. The most active compounds in this series are 7, 9 and 20, cent percent active in preventing implantation in rats at 2.5 mgkg(-1) dose.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Embryo Implantation / drug effects*
  • Estrogen Antagonists / chemical synthesis*
  • Estrogen Antagonists / pharmacology
  • Female
  • Ligands
  • Models, Molecular
  • Naphthols / chemical synthesis*
  • Naphthols / pharmacology*
  • Organ Size / drug effects
  • Rats
  • Receptors, Estrogen / agonists
  • Receptors, Estrogen / antagonists & inhibitors
  • Structure-Activity Relationship
  • Uterus / drug effects

Substances

  • Estrogen Antagonists
  • Ligands
  • Naphthols
  • Receptors, Estrogen