Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375545 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
The first examples of thioether-substituted benzonitriles as potential soft-drug androgen receptor antagonists are reported. A number of 4-(alkylthio)- and of 4-(arylthio)-benzonitrile analogs were evaluated in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro binding and cellular activities were evaluated for topical in vivo efficacy in the Golden Syrian hamster ear model. Analogs from both the 4-(alkylthio)- and of 4-(arylthio)-benzonitrile series showed moderate reduction of wax esters in vivo.
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Authors
Lorna Mitchell, Zhi Wang, Lain-Yen Hu, Catherine Kostlan, Matthew Carroll, Danielle Dettling, Daniel Du, David Pocalyko, Kimberly Wade,