Article
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Bioorganic & medicinal chemistry letters - 17 Jan 2005
Salvati Mark E, Balog Aaron, Wei Donna D, Pickering Dacia, Attar Ricardo M, Geng Jieping, Rizzo Cheryl A, Hunt John T, Gottardis Marco M, Weinmann Roberto, Martinez Rogelio
Abstract excerpt
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...
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