Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2731-6. doi: 10.1016/s0960-894x(98)00482-x.

Abstract

A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells.

MeSH terms

  • Humans
  • Molecular Conformation
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Receptors, Progesterone / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Quinolines
  • Receptors, Progesterone