MEL-6

MEL-6 is an investigational **small-molecule androgen receptor antagonist** being studied as a potential therapy for **prostate cancer**, particularly tumors resistant to currently used androgen receptor antagonists. It was reported from preclinical medicinal chemistry work as a novel scaffold that binds the androgen receptor ligand-binding pocket and induces an antagonistic receptor conformation, including activity against resistance-associated androgen receptor mutations such as **W741C, T877A, and F876L-T877A**. In cell-based studies, MEL-6 showed antiproliferative effects in androgen receptor-positive prostate cancer models, inhibited androgen-regulated transcriptional programs, and demonstrated relative selectivity versus other steroid receptors. The published work also noted that MEL-6 exists as multiple stereoisomers, with one enantiomeric pair responsible for the observed antiandrogenic activity, and that later analog optimization improved metabolic stability beyond the parent MEL-6 scaffold.

Other names

3-Methoxy-N-[1-methyl-2-(4-phenyl-1-piperazinyl)-2-(2-thienyl)ethyl]benzamide