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
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; 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
相关论文
共 50 条
[21]   Design, synthesis, crystal structure, biological evaluation and molecular docking studies of carbazole-arylpiperazine derivatives [J].
Xu, Wei ;
Huang, Junjun ;
Shao, Binhao ;
Xu, Xingjie ;
Jiang, Renwang ;
Yuan, Mu .
BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 24 (21) :5565-5572
[22]   Synthesis and biological evaluation of multimodal monoaminergic arylpiperazine derivatives with potential antidepressant profile [J].
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
[23]   Synthesis of novel heptaplatin derivatives and evaluation of their ability to inhibit proliferation of cancer cell lines [J].
W. Xu ;
D. C. Wang .
Russian Journal of General Chemistry, 2016, 86 :939-943
[24]   Synthesis of novel heptaplatin derivatives and evaluation of their ability to inhibit proliferation of cancer cell lines [J].
Xu, W. ;
Wang, D. C. .
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2016, 86 (04) :939-943
[25]   Design, Synthesis and Biological Evaluation of Novel Catalpol Derivatives as Potential Pancreatic Cancer Inhibitors [J].
Kong, Yuanfang ;
Liu, Shuanglin ;
Wang, Shaopei ;
Xu, Jindan ;
Hu, Yulong ;
Jiang, Shiqing ;
Dong, Chunhong .
CHEMISTRY-AN ASIAN JOURNAL, 2023, 18 (12)
[26]   Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists [J].
Jin, Jing ;
Wang, Xiao-Bing ;
Kong, Ling-Yi .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (03) :909-911
[27]   Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents [J].
Chen, Jing ;
Du, Wenting ;
Tao, Xuefen ;
Huang, Jiawei ;
Song, Yuliang ;
Ying, Huazhou .
LETTERS IN DRUG DESIGN & DISCOVERY, 2013, 10 (09) :879-885
[28]   Design, Synthesis, and Biological Evaluation of Axitinib Derivatives [J].
Wei, Na ;
Liang, Jianqing ;
Peng, Shengming ;
Sun, Qiang ;
Dai, Qiuyun ;
Dong, Mingxin .
MOLECULES, 2018, 23 (04)
[29]   Design, Synthesis, Biological Evaluation, and Molecular Dynamics Studies of Novel Lapatinib Derivatives [J].
Elkamhawy, Ahmed ;
Son, Seohyun ;
Lee, Hwa Young ;
El-Maghrabey, Mahmoud H. ;
El Hamd, Mohamed A. ;
Alshammari, Saud O. ;
Abdelhameed, Abeer A. ;
Alshammari, Qamar A. ;
Abdeen, Ahmed ;
Ibrahim, Samah F. ;
Mahdi, Wael A. ;
Alshehri, Sultan ;
Alnajjar, Radwan ;
Choi, Won Jun ;
Al-Karmalawy, Ahmed A. ;
Lee, Kyeong .
PHARMACEUTICALS, 2023, 16 (01)
[30]   Novel curcumin derivatives as potential anticancer agents: design, synthesis and biological evaluation [J].
Liu, Wenqing ;
Yang, Sha ;
Pan, Yongchun ;
Wei, Bingliang ;
Liu, Mingsong ;
Zhu, Huajie ;
Xu, Zhidong .
NATURAL PRODUCT RESEARCH, 2024,