Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell LinesReportar como inadecuado




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Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China



These authors contributed equally to this work.





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Abstract 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. View Full-Text

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





Autor: Hong Chen †, Xue Liang †, Fang Xu, Bingbing Xu, Xuelan He, Biyun Huang and Mu Yuan *

Fuente: http://mdpi.com/



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