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

页码：285 / 287

页数：3

共 50 条

[31] Design, Synthesis and Evaluation of N13-Substituted Evodiamine Derivatives against Human Cancer Cell Lines
Song, Senchuan
Chen, Zhiyong
Li, Shaoxue
Huang, Yanmin
Wan, Yiqian
Song, Huacan
MOLECULES, 2013, 18 (12): : 15750 - 15768
[32] Design, synthesis and cytotoxicity studies of dithiocarbamate ester derivatives of emetine in prostate cancer cell lines
Akinboye, Emmanuel S.
Bamji, Zebalda D.
Kwabi-Addo, Bernard
Ejeh, David
Copeland, Robert L.
Denmeade, Samuel R.
Bakare, Oladapo
BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 23 (17) : 5839 - 5845
[33] Synthesis and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile
Zheng, Jiefang
Zhou, Liping
Gong, Xudong
Yang, Feipu
Cheng, Jiaxin
Ma, Rui
Wu, Chunhui
Xu, Zhijian
Zhu, Weiliang
He, Yang
Shen, Jingshan
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2024, 275
[34] Synthesis of novel heptaplatin derivatives and evaluation of their ability to inhibit proliferation of cancer cell lines
W. Xu
D. C. Wang
Russian Journal of General Chemistry, 2016, 86 : 939 - 943
[35] Design, Synthesis and Biological Evaluation of Novel Catalpol Derivatives as Potential Pancreatic Cancer Inhibitors
Kong, Yuanfang
Liu, Shuanglin
Wang, Shaopei
Xu, Jindan
Hu, Yulong
Jiang, Shiqing
Dong, Chunhong
CHEMISTRY-AN ASIAN JOURNAL, 2023, 18 (12)
[36] Synthesis of novel heptaplatin derivatives and evaluation of their ability to inhibit proliferation of cancer cell lines
Xu, W.
Wang, D. C.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2016, 86 (04) : 939 - 943
[37] Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists
Jin, Jing
Wang, Xiao-Bing
Kong, Ling-Yi
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (03) : 909 - 911
[38] Design, Synthesis, and Biological Evaluation of Some Novel Retinoid Derivatives
Konyar, Dilan
Foto, Egemen
Foto, Fatma Zilifdar
Buyukbingol, Mehmet Erdem
LETTERS IN DRUG DESIGN & DISCOVERY, 2024, 21 (14) : 2926 - 2938
[39] Design, Synthesis, and Biological Evaluation of a Novel Series of Pirfenidone Derivatives
Yong Gengga Sangmao
Wei Li
Liming Wang
Zhigang Jin
Shufan Yang
Congdi Yin
Hongjun Chen
Russian Journal of Bioorganic Chemistry, 2022, 48 : 430 - 437
[40] Design, synthesis and biological evaluation of novel betulinic acid derivatives
Shengjie Yang
Na Liang
Hu Li
Wei Xue
Deyu Hu
Linhong Jin
Qi Zhao
Song Yang
Chemistry Central Journal, 6

← 1 2 3 4 5 →