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

被引：11
作者：
Chen, Hong [1 ,2 ]
Xu, Fang [2 ]
Xu, Bing-Bing [2 ]
Xu, Jing-Yi [2 ]
Shao, Bin-Hao [2 ]
Huang, Bi-Yun [2 ]
Yuan, Mu [2 ]
机构：
[1] Luoyang Normal Univ, Coll Chem & Chem Engn, Luoyang 471022, Peoples R China
[2] Guangzhou Med Univ, Pharmaceut Res Ctr, Guangzhou 510182, Guangdong, Peoples R China
来源：
CHINESE CHEMICAL LETTERS | 2016年 / 27卷 / 02期
基金：
美国国家科学基金会; 中国博士后科学基金;
关键词：
Synthesis; Arylpiperazine derivatives; Cytotoxic activity; CCK-8; Structure-activity relationship; ACUTE LYMPHOBLASTIC-LEUKEMIA; ALPHA(1)-ADRENOCEPTOR ANTAGONISTS; NAFTOPIDIL; DRUGS; CHEMOTHERAPY; HYPERPLASIA; TAMSULOSIN; MANAGEMENT; RESISTANCE; EFFICACY;
D O I：
10.1016/j.cclet.2015.09.016
中图分类号：
O6 [化学];
学科分类号：
0703 ;
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 8, 10, 13, 17 and 20 exhibited strong cytotoxic activities against the tested cancer cell lines (IC50 <3 mu mol/L). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells WPMY-1. The structure-activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data. (C)2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
引用
收藏
页码：277 / 282
页数：6
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