Activity of Steroid 4 and Derivatives 4a–4f as Inhibitors of the Enzyme 5α-Reductase Type 1

    June 2018 in “ Bioorganic & medicinal chemistry ”
    Yazmín Arellano, Eugene Bratoeff, Yvonne Heuze, Marisol Bravo, Juan Soriano, Marisa Cabeza
    TLDR Compounds 4, 4b, and 4c effectively inhibit an enzyme linked to testosterone conversion without significant toxicity.
    The study synthesized and tested seven steroid derivatives (4, 4a–4f) as inhibitors of the enzyme 5α-reductase type 1 (5α-R1), which is predominant in metastatic prostate bone tumors. In vitro assays showed that compounds 4, 4b, and 4c effectively inhibited 5α-R1 activity. In vivo experiments on gonadectomized hamsters demonstrated that these derivatives reduced the diameter of flank glands and the weight of prostate and seminal vesicles without significant toxicity. The derivatives exhibited improved plasma half-life due to their stability against hydrolysis, with compound 4e showing the greatest pharmacological effect. The study concluded that these derivatives could serve as potential prodrugs for treating metastatic prostate cancer.
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