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Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Salvati ME,Balog A,Wei DD,Pickering D,Attar RM,Geng J,Rizzo CA,Hunt JT,Gottardis MM,Weinmann R,Martinez R

doi

10.1016/j.bmcl.2004.10.051

subject

Has Abstract

pub_date

2005-01-17 00:00:00

pages

389-93

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01292-2

journal_volume

15

pub_type

杂志文章

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