Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines

Molecules

Hong Chen¹  Xue Liang¹  Fang Xu²  Bingbing Xu²  Xuelan He²  Biyun Huang² 

[1] Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China;

关键词: synthesis;    arylpiperazine derivatives;    cytotoxic activity;    CCK-8;    structure-activity relationship;   

DOI  :  10.3390/molecules190812048

来源: mdpi

【 摘 要 】

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 9 and 15 exhibited strong cytotoxic activities against LNCaP cells (IC₅₀ < 5 μM), and compound 8 (IC₅₀ = 8.25 μM) possessed the most potent activity against DU145 cells. However, these compounds also exhibited cytotoxicity towards 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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.