Title of article
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus
Author/Authors
Mark E. Salvati، نويسنده , , Aaron Balog، نويسنده , , Donna D. Wei، نويسنده , , Dacia Pickering، نويسنده , , Ricardo M. Attar، نويسنده , , Jieping Geng، نويسنده , , Cheryl A. Rizzo، نويسنده , , John T. Hunt، نويسنده , , Marco M. Gottardis، نويسنده , , Roberto Weinmann، نويسنده , , Rogelio Martinez، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
389
To page
393
Abstract
A novel series of isoindoledione based compounds were identified as potent antagonists of the androgen receptor (AR). SAR around this series revealed dramatic differences in binding and function in mutant variants (MT) of the AR as compared to the wild type (WT) receptor. Optimization of the aniline portion revealed substitution patterns, which yielded potent antagonist activity against the WT AR as well as the MT AR found in the LNCaP and PCa2b human prostate tumor cell lines.
Keywords
androgen receptor , prostate cancer , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795213
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