Application of fluorine-containing non-steroidal anti-androgen compounds in treating prostate cancer

Prostate cancer is one of leading causes of male deaths in Europe and US and is becoming a dramatically increasing malignancy in Asian countries including China. This disease is related to hormone malfunction linked with androgen receptor cell signaling. Targeting androgen receptor has been a major strategy for treating this disease. Among these treatments, small molecules such as flutamide, bicalutamide and newly FDA-approved MDV3100 are the mainstay of drugs in clinical use. Interestingly, all of them are fluorine-containing compounds, indicating a unique role of fluorine atom on treating this cancer. In this mini-review, we summarize the prostate cancer-related cell signaling, chemistry and mechanisms of action of these drugs, highlighting the importance of fluorine chemistry on treating prostate cancer.