FAR11

FAR11 is a small molecule androgen receptor (AR) antagonist belonging to a series of 4,4-dimethylimidazolidin-2-one pharmacophore-based compounds. It was designed as a flexible analog of second-generation AR antagonists like enzalutamide, specifically replacing the rigid thiohydantoin pharmacophore with a 4,4-dimethylimidazolidin-2-one moiety and introducing a methylene spacer to increase conformational flexibility. FAR11 was developed to address resistance mechanisms in prostate cancer, such as castration-resistant prostate cancer (CRPC), by inhibiting AR signaling which remains fundamental to tumor growth even under androgen deprivation. In preclinical studies, the series was evaluated for in vitro activity against the androgen-dependent LNCaP prostate cancer cell line.