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

被引：25

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

页码：285 / 287

页数：3

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