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.
作者信息
Kong J W, Hamann L G, Ruppar D A, Edwards J P, Marschke K B, Jones T K
机构信息
Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2000 Mar 6;10(5):411-4. 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.
摘要
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