TLDR Smaller substituents at C-17 enhance the inhibitory activity of progesterone derivatives on 5alpha-reductase.
The study synthesized and evaluated four new progesterone derivatives as 5alpha-reductase inhibitors, using both in vivo and in vitro methods. In vivo tests on gonadectomized male hamsters showed that these compounds, when combined with testosterone, significantly reduced prostate weight compared to testosterone alone. In vitro tests using human prostate homogenates revealed varying IC50 values, indicating differing levels of inhibitory activity. Compound 15, with an acetoxy substituent, showed the highest inhibitory activity with an IC50 of 6.3 x 10(-11) M, while compound 12, with a free alcohol, showed much lower activity. The study concluded that the inhibitory activity was influenced by the steric effect of the substituent at C-17, with smaller substituents enhancing activity.
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January 2002 in “Chemical & pharmaceutical bulletin/Chemical and pharmaceutical bulletin” New pregnane derivatives were more effective than finasteride at inhibiting a key enzyme for male pattern baldness.
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