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

作者：Chen, Hong; Xu, Fang; Liang, Xue; Xu, Bing-Bing; Yang, Zong-Lin; He, Xue-Lan; Huang, Bi-Yun; Yuan, Mu^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(2): 285-287.

DOI：10.1016/j.bmcl.2014.11.049

• Synthesis
• Arylpiperazine derivatives
• Cytotoxic activity
• CCK-8
• Structure-activity relationship

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 10, 24 and 29 exhibited strong cytotoxic activities against LNCaP cells (IC50 < 3 mu M). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells RWPE-1. The structure-activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data.

• 出版日期2015-1-15
• 单位广州医科大学