The search for nonsteroidal antiandrogens that will block the pharmacological effects of testosterone, led to the development of compounds like flutamide, nilutamide, and (R,S)-bicalutamide , which are widely used for the treatment of metastatic prostate cancer ( Scheme 1). [1], [2], [3] and [4] The commonly accepted structure–activity relationship borne out of these ligands suggest the importance of an electron deficient aromatic ring, branched alkyl group α to the amidic ...