Author/Authors :
Jennifer A. Van Camp، نويسنده , , Lain-Yen Hu، نويسنده , , Catherine Kostlan، نويسنده , , Bruce Lefker، نويسنده , , Jie Li، نويسنده , , Lorna Mitchell، نويسنده , , Zhi Wang، نويسنده , , Wen-Song Yue، نويسنده , , Matthew Carroll، نويسنده , , Danielle Dettling، نويسنده , , Daniel du Plessis، نويسنده , , David Pocalyko، نويسنده , , Kimberly Wade، نويسنده ,
Abstract :
A series of substituted 4-aryl-2-trifluoromethylbenzonitrile analogs were evaluated in the human androgen receptor binding and cellular functional assays. Analogs with sufficient in vitro binding and cellular potency (IC50 < 200 nM) were tested in the progesterone receptor binding assay for selectivity and in the Golden Syrian hamster ear model for in vivo efficacy. Within the series, compound 4e was identified to be the most active analog in vivo (wax ester inhibition = 86%).
