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

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.