In Vivo and In Vitro Effect of Novel 4,16-Pregnadiene-6,20-Dione Derivatives as 5α-Reductase Inhibitors

    Eugene Bratoeff, Marisa Cabeza, Victor Pérez-Ornelas, Sergio Recillas‐Morales, Ivonne Heuze
    TLDR The new compounds may be more effective and cheaper than current treatments for conditions like baldness.
    The study explored the synthesis and effects of five novel steroid derivatives as 5α-reductase inhibitors, which are crucial for treating androgen-dependent conditions like baldness. These compounds, featuring an ester moiety at C-3 and conjugated double bonds at C-4 and C-16, were tested in both in vivo and in vitro settings. The results showed that these derivatives had higher activity than finasteride, a common treatment, with compound 11b exhibiting a significantly lower IC50 of 1.8 nM compared to finasteride's 8.5 nM. In vivo, they effectively reduced prostate weight in testosterone-treated, castrated hamsters. The presence of halogens enhanced their activity without binding to androgen receptors, suggesting fewer side effects. These findings suggested that these compounds could be more effective and cost-efficient alternatives for treating androgen-related conditions.
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