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.
L G Hamann  1 ,  D T Winn ,  C L Pooley ,  C M Tegley ,  S J West ,  L J Farmer ,  L Zhi ,  J P Edwards ,  K B Marschke ,  D E Mais ,  M E Goldman ,  T K Jones
Affiliations
  • 1. Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
PMID: 9873612 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.