2. Academic Validation
  3. 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

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

Affiliation

  • 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.

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