5α-Reductase Inhibitors, Antiviral and Anti-Tumor Activities of Some Steroidal Cyanopyridinone Derivatives

In the 2012 study, researchers synthesized seventeen steroidal cyanopyridinone derivatives and assessed their 5α-reductase inhibitory, antiviral, and anti-tumor properties. The compounds were found to be less toxic than the reference drug Prednisolone, except for one (3b). They exhibited potent inhibition of 5α-reductase, an enzyme linked to benign prostatic hyperplasia and androgenic alopecia, and showed cytotoxicity against two human prostate cancer cell lines, LNCaP and PC-3. The derivatives also demonstrated strong antiviral effects against HIV and HCV. The study highlighted that some compounds had superior activities compared to reference drugs, indicating their potential as therapeutic agents. The document also detailed the compounds' antiviral and anti-tumor effects against influenza A virus strains H1N1 and H3N2, and various cancer cell lines. It was found that certain structural features, such as a 33-hydroxyl group and fluoride substitution, enhanced their activity. The cytotoxicity IC50 values for the compounds were provided, with bicalutamide as the reference standard. The study concluded that these compounds show significant promise as 5α-reductase inhibitors, antivirals, and anti-tumor agents. Specific data on the number of people in the study or the exact values of the inhibitory activities were not provided in the summary.