Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines

  • Bioorg Med Chem Lett. 2000 Mar 6;10(5):411-4. doi: 10.1016/s0960-894x(00)00010-x.
J W Kong  1 ,  L G Hamann ,  D A Ruppar ,  J P Edwards ,  K B Marschke ,  T K Jones
Affiliations
  • 1. Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
PMID: 10743937 DOI: 10.1016/s0960-894x(00)00010-x
Abstract

A series of nonsteroidal human Androgen Receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethylpyrido[3,2-g]quin olines was synthesized. Compounds in this series were tested for the ability to bind to hAR and inhibit hAR-dependent transcription in a mammalian cellular background.