Title of article
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5529
To page
5532
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%).
Keywords
Androgen receptor antagonists , Sebum production inhibitors , Biaryl analogs
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798647
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