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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    TLDR Scientists made a chemical (compound 4e) that can be applied on skin to reduce oil production, which can help with acne, but it might cause skin sensitivity to light.
    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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