Synthesis and In Vitro Evaluation of 4-Substituted N-(1,1-Dimethylethyl)-3-Oxo-4-Androstene-17β-Carboxamides as 5α-Reductase Inhibitors and Antiandrogens

In the 1995 study, researchers synthesized four new compounds and evaluated their effectiveness as inhibitors of the 5α-reductase enzymes, which are involved in converting testosterone to dihydrotestosterone (DHT), a hormone linked to various androgen-sensitive conditions. The compounds displayed weak inhibition of type I 5α-reductase, with IC50 values greater than or equal to 700 nM, but showed intermediate inhibitory activity on type II 5α-reductase, with IC50 values ranging from 172 to 437 nM. Additionally, the compounds exhibited strong antiandrogenic properties, inhibiting DHT-induced proliferation of androgen-sensitive cancer cells with IC50 values between 170 and 279 nM. The study concluded that these compounds could potentially be used to treat diseases like benign prostatic hyperplasia, prostate cancer, and androgenic alopecia due to their moderate inhibition of type II 5α-reductase and potent antiandrogenic effects.