Development of a Benzothiazole Scaffold-Based Androgen Receptor N-Terminal Inhibitor for Treating Androgen-Responsive Prostate Cancer

Investigators described the identification of 2-(4-fluorophenyl)-5-(trifluoromethyl)-1,3-benzothiazole, a small molecule that inhibits BAG1L– androgen receptor (AR) N-terminal domain (NTD) interaction, attenuated BAG1L-mediated AR NTD activity, downregulated AR target gene expression, and inhibited proliferation of AR-positive prostate cancer cells.