FAR06

FAR06 is a small molecule androgen receptor (AR) antagonist designed as part of a series of 4,4-dimethylimidazolidin-2-one pharmacophore-based compounds. It was developed to target AR signaling in the treatment of prostate cancer, particularly to overcome resistance mechanisms associated with castration-resistant prostate cancer (CRPC). Structurally, FAR06 replaces the rigid thiohydantoin pharmacophore found in second-generation antagonists like enzalutamide with a more flexible 4,4-dimethylimidazolidin-2-one core and incorporates a methylene group between the pharmacophore and an aromatic ring to further increase molecular flexibility. Despite lacking the amide functional group typically found in this class of AR antagonists, FAR06 demonstrates potent in vitro activity against the androgen-dependent LNCaP prostate cancer cell line, with an IC50 value of 0.801 μM, which is nearly identical to the potency of enzalutamide.