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

被引：23
|
作者：
Chen, Hong [1 ]
Xu, Fang [1 ]
Liang, Xue [1 ]
Xu, Bing-Bing [1 ]
Yang, Zong-Lin [1 ]
He, Xue-Lan [1 ]
Huang, Bi-Yun [1 ]
Yuan, Mu [1 ]
机构：
[1] Guangzhou Med Univ, Pharmaceut Res Ctr, Guangzhou 510182, Guangdong, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 02期
基金：
中国博士后科学基金; 美国国家科学基金会;
关键词：
Synthesis; Arylpiperazine derivatives; Cytotoxic activity; CCK-8; Structure-activity relationship; URINARY-TRACT-SYMPTOMS; ALPHA(1)-ADRENOCEPTOR ANTAGONISTS; NAFTOPIDIL; LIGANDS; POTENT; TAMSULOSIN; MANAGEMENT; RESISTANCE; DISCOVERY; EFFICACY;
D O I：
10.1016/j.bmcl.2014.11.049
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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 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. (C) 2014 Published by Elsevier Ltd.
引用
收藏
页码：285 / 287
页数：3
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