Preparation of 4-Aryl-2-Trifluoromethylbenzonitrile Derivatives as Androgen Receptor Antagonists for Topical Suppression of Sebum Production

    August 2007 in “ Bioorganic & Medicinal Chemistry Letters ”
    Jennifer A. Van Camp, Lain-Yen Hu, Catherine R. Kostlan, Bruce Allen Lefker, Jie Li, Lorna Helen Mitchell, Zhi Wang, Wen Yue, Matthew Carroll, Danielle Dettling, Daniel K. Du, David Pocalyko, Kimberly Jane Wade
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    Studysummary This study found that among the tested analogs, compound 4e was the most effective in inhibiting wax esters in vivo in the Golden Syrian hamster ear model. Our plain-language summary of this paper — not a Tressless recommendation.
    In 2007, researchers at Pfizer Global Research and Development created a series of 4-aryl-2-trifluoromethylbenzonitrile analogs, which are androgen receptor antagonists, to topically reduce sebum production, a factor contributing to acne vulgaris infections. These analogs were tested in human androgen receptor binding and cellular functional assays. The most effective analog was compound 4e, which inhibited 86% of wax ester, directly reducing sebum production. However, this compound showed potential for phototoxicity. The study concluded that while compound 4e was the most potent, increasing its steric bulk resulted in a loss of receptor binding.
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