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

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

Affiliation

  • 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.

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