Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines

A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds 8, 10, 13, 17 and 20 exhibited strong cytotoxic activities against the tested cancer cell lines (IC50 <3 μmol/L). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells WPMY-1. The structure–activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data.

Graphical abstractA novel series of arylpiperazine derivatives was synthesized and evaluated for their cytotoxic activity against three human prostate cancer cell lines. Among all, compounds 8, 10 and 20 exhibited strong cytotoxic activities against the tested cancer cells.Figure optionsDownload full-size imageDownload as PowerPoint slide