Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide

Taking inspiration from the current leading antiandrogen used to treat prostate cancer, Bicalutamide (Casodex®), six triazole-derived analogues were synthesised and evaluated as androgen receptor (AR) antagonists. The synthesis for these compounds is very efficient, being five steps long and giving overall yields up to 85%. Docking of these compounds into the human AR (T877A mutant) showed encouraging interactions with the receptor and a comparison to established AR antagonists is presented. Evaluation of these compounds in vitro against hormone sensitive (LNCaP) and hormone independent (PC3) cells showed promising IC50 values of down to 34 μM and 29 μM, respectively.