Synthesis and Cytotoxic Activity 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 9 and 15 exhibited strong cytotoxic activities against LNCaP...

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Autores principales: Chen, Hong, Liang, Xue, Xu, Fang, Xu, Bingbing, He, Xuelan, Huang, Biyun, Yuan, Mu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271825/
https://www.ncbi.nlm.nih.gov/pubmed/25120056
http://dx.doi.org/10.3390/molecules190812048
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author Chen, Hong
Liang, Xue
Xu, Fang
Xu, Bingbing
He, Xuelan
Huang, Biyun
Yuan, Mu
author_facet Chen, Hong
Liang, Xue
Xu, Fang
Xu, Bingbing
He, Xuelan
Huang, Biyun
Yuan, Mu
author_sort Chen, Hong
collection PubMed
description 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 (IC(50) < 5 μM), and compound 8 (IC(50) = 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.
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spelling pubmed-62718252018-12-27 Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines Chen, Hong Liang, Xue Xu, Fang Xu, Bingbing He, Xuelan Huang, Biyun Yuan, Mu Molecules Article 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 (IC(50) < 5 μM), and compound 8 (IC(50) = 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. MDPI 2014-08-12 /pmc/articles/PMC6271825/ /pubmed/25120056 http://dx.doi.org/10.3390/molecules190812048 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Chen, Hong
Liang, Xue
Xu, Fang
Xu, Bingbing
He, Xuelan
Huang, Biyun
Yuan, Mu
Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title_full Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title_fullStr Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title_full_unstemmed Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title_short Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
title_sort synthesis and cytotoxic activity evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271825/
https://www.ncbi.nlm.nih.gov/pubmed/25120056
http://dx.doi.org/10.3390/molecules190812048
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