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Authors Salvati ME, Balog A, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Hunt JT, Gottardis MM, Weinmann R, Martinez R
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Journal Bioorg. Med. Chem. Lett. Volume: 15 Issue: 2 Pages: 389-93
Publish Date 2005 Jan 17
PubMed ID 15603960

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. Copyright © 2016 The Board of Regents of the University of Wisconsin System