Synthesis and in vitro anti-proliferative activity of racemic trifluoro-Casodex® (Bicalutamide)

The trifluoro analogue 1 of Casodex® was synthesized in racemic form, according to a strategy based on the use of trifluoropyruvate as a key starting material. This compound showed significant in vitro anti-proliferative activity on the human prostate cancer cell line LNCaP