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Molecules 2014, 19(8), 12048-12064; doi:10.3390/molecules190812048

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

Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Received: 7 July 2014 / Revised: 4 August 2014 / Accepted: 6 August 2014 / Published: 12 August 2014
(This article belongs to the Section Organic Synthesis)
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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
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Chen, H.; Liang, X.; Xu, F.; Xu, B.; He, X.; Huang, B.; Yuan, M. Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines. Molecules 2014, 19, 12048-12064.

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