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 ,
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.
