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

• Published in: Journal of fluorine chemistry Vol. 161; pp. 1 - 10
• Main Authors: Yang, Xiaoping, Guan, Aiying
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.05.2014
• Subjects: Androgen receptor; Cancer; Drugs; Fluorine; Fluorine-containing small molecule; Males; Medical services; Non-steroidal antiandrogen; Prostate; Prostate cancer; Receptors; Strategy; Non-steroidal antiandrogen; Prostate cancer; Androgen receptor; Fluorine-containing small molecule
• ISSN: 0022-1139; 1873-3328
• DOI: 10.1016/j.jfluchem.2014.02.001

H&E stain represents prostate cancer tissue with blue ribbon as the symbol of prostate cancer. The chemical structure of a very recently approved enzalutamide drug, which blocks the androgen receptor signaling with highlighting fluorine atoms, is presented in this cartoon. 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.