Relative Binding Affinity of Novel Steroids to Androgen Receptors in Hamster Prostate

In the 2005 study, researchers synthesized and tested the antiandrogenic activity of nine novel steroidal compounds on androgen receptors in hamster prostate. The compounds included four aromatic esters, one aliphatic ester based on the pregnadiene structure, and four valeroyloxy esters based on the pregnene skeleton. The binding affinity was measured using competitive binding assays, with compounds 10a-10c showing the highest affinities. In vivo tests with gonadectomized male hamsters demonstrated that all steroidal derivatives reduced prostate gland weight when treated with DHT, indicating their antagonistic effect on the androgen receptor. The pregnadiene derivatives showed higher antiandrogenic activity than the pregnene-based steroids. The study concluded that these novel compounds are effective androgen receptor antagonists and suggested that increased conjugation in the steroidal molecule enhances antiandrogenic activity. The in vivo experiments involved 12 groups of 4 animals each.