Synthesis and Biological Evaluation of Novel Unsaturated Carboxysteroids as Human 5α-Reductase Inhibitors: A Legitimate Approach

In this study, researchers synthesized novel steroidal compounds and evaluated their potential as 5α-reductase inhibitors, which are relevant for treating conditions like hair loss. The compounds were tested both in vitro using human embryonic kidney cells and in vivo using a rat prostate weighing method. Notably, compounds 21–23 and 25 demonstrated potent inhibition of the 5α-reductase II enzyme with IC50 values of 54.1 ± 9.5, 22.1 ± 2.4, 72.8 ± 2.3, and 26.5 ± 4.4 nM, respectively, compared to Finasteride's 30.3 nM. These compounds also significantly reduced rat prostate weight, indicating their potential effectiveness.