Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production |
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Authors: | Van Camp Jennifer A Hu Lain-Yen Kostlan Catherine Lefker Bruce Li Jie Mitchell Lorna Wang Zhi Yue Wen-Song Carroll Matthew Dettling Danielle Du Daniel Pocalyko David Wade Kimberly |
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Affiliation: | Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. jennifer_vancamp@yahoo.com |
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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 (IC(50)<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 4 e was identified to be the most active analog in vivo (wax ester inhibition=86%). |
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