Design, Synthesis, and Biological Evaluation of Novel Androst-3,5-Diene-3-Carboxylic Acid Derivatives as Inhibitors of 5α-Reductase Type 1 and 2
June 2017
in “
Steroids
”
TLDR New chemical compounds were made that effectively block an enzyme linked to prostate growth.
In this study, researchers designed and synthesized a series of novel steroidal androst-3,5-diene-3-carboxylic acid derivatives to inhibit 5α-reductase type 1 and 2, enzymes involved in the biosynthesis of dihydrotestosterone (DHT). The compounds were evaluated for their inhibitory activity both in vitro and in vivo. Results indicated that most derivatives exhibited good inhibitory activities, particularly those with 2′-substituted aniline groups (compounds 16a, 16h-16j). The study suggested that these novel compounds could potentially serve as effective treatments for conditions like benign prostatic hyperplasia (BPH) by reducing DHT levels.
