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

J W Kong; L G Hamann; D A Ruppar; J P Edwards; K B Marschke; T K Jones

doi:10.1016/s0960-894x(00)00010-x

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.

Authors

J W Kong¹, L G Hamann, D A Ruppar, J P Edwards, K B Marschke, T K Jones

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.

MeSH terms

Androgen Antagonists / chemical synthesis*
Androgen Antagonists / pharmacology
Androgen Receptor Antagonists*
Androgens / metabolism
Animals
COS Cells
Humans
Pyridones / chemical synthesis*
Pyridones / chemistry*
Pyridones / pharmacology
Quinolines / chemical synthesis*
Quinolines / pharmacology
Transcription, Genetic / drug effects

Substances

Androgen Antagonists
Androgen Receptor Antagonists
Androgens
Pyridones
Quinolines