FAR05

FAR05 is an experimental small molecule androgen receptor (AR) antagonist belonging to a series of 4,4-dimethylimidazolidin-2-one derivatives (FAR01-FAR11). It was designed to target prostate cancer, including castration-resistant prostate cancer (CRPC), by inhibiting AR signaling. The molecule features a flexible 4,4-dimethylimidazolidin-2-one pharmacophore, which serves as a structural alternative to the rigid thiohydantoin ring found in the second-generation AR antagonist enzalutamide. FAR05 was developed to explore the impact of electronic effects and intramolecular non-covalent interactions on AR antagonistic activity. Unlike many conventional AR antagonists, this class of molecules lacks an amide functional group and incorporates an additional methylene group between the pharmacophore and one of the aromatic rings to increase molecular flexibility.