High‐throughput screening for anti‐tumor activity in different prostate cancer cell models with either AR expression or inactivation, which identifies six potential anti‐tumor molecules among which, subsequent cytotoxicity testing revealed that an analog, L14, derived from ezetimibe as a marketed drug previously used for intestinal cholesterol and phytosterol absorption, exhibited the best anti‐tumor activity and in vitro specificity among the six molecules. This evidence concerns the gene AR and neoplasm.