QSAR Analysis of a Series of Hydantoin-Based Androgen Receptor Modulators and Corresponding Binding Affinities

This study designed a novel model for 5a-reductase enzyme inhibitors using pharmacophore and 3D QSAR techniques, potentially allowing for improved prediction and development of drug therapies targeting benign prostatic hyperplasia.

This study found that a novel thiohydantoin derivative, 3a, effectively inhibited androgen receptor activity in LNCaP cells and showed promising in vivo results by reducing testosterone-induced prostate changes, outperforming finasteride in mitigating prostate index and histopathological alterations.

This study found that arylhydantoin and arylthiohydantoin derivatives with hydroxybutyl or methyl side-chains showed superior androgen receptor binding affinity and may serve as promising radioiodinated AR ligands.

This study identified the N-(iodopropenyl) derivative 13 as a promising candidate for development as a radioiodinated androgen receptor ligand due to its binding affinity.