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

共 50 条

[41] Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors [J].

Ma, Tianyi ;

Huang, Min ;

Li, Aihua ;

Zhao, Feng ;

Li, Deyi ;

Liu, Dan ;

Zhao, Linxiang .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2019, 29 (14) :1859-1863

[42] Design, synthesis and biological evaluation of honokiol derivatives as influenza neuraminidase inhibitors [J].

Lin, Ding ;

Yi, Yang-Jie ;

Xiao, Meng-Wu ;

Chen, Jia ;

Ye, Jiao ;

Hu, Ai-Xi ;

Lian, Wen-Wen ;

Liu, Ai-Lin ;

Du, Guan-Hua .

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH, 2019, 21 (11) :1052-1067

[43] Synthesis of Resveratrol Acrylamides Derivatives and Biological Evaluation of their Anti-Proliferative Effect on Cancer Cell Lines [J].

Ruan, Ban-Feng ;

Wang, Si-Qi ;

Ge, Xiao-Lin ;

Yao, Ri-Sheng .

LETTERS IN DRUG DESIGN & DISCOVERY, 2014, 11 (01) :2-9

[44] Design, synthesis, and biological activity of a novel series of benzofuran derivatives against oestrogen receptor-dependent breast cancer cell lines [J].

Jin, Li-Ping ;

Xie, Qian ;

Huang, Er-Fang ;

Wang, Lin ;

Zhang, Bing-Qi ;

Hu, Jian-Shu ;

Wan, David Chi-Cheong ;

Jin, Zhe ;

Hu, Chun .

BIOORGANIC CHEMISTRY, 2020, 95

[45] Design, Synthesis and Biological Evaluation of Novel Imidazolone Derivatives as Dipeptidyl Peptidase 4 Inhibitors [J].

Liu, Yang ;

Jiang, Chaoyi ;

Wu, Haoshu ;

Wu, Peng ;

Si, Meimei ;

Hu, Yongzhou ;

Liu, Tao .

MEDICINAL CHEMISTRY, 2013, 9 (07) :938-946

[46] Design, Synthesis, and Biological Evaluation of Novel Evodiamine Derivatives as Potential Antihepatocellular Carcinoma Agents [J].

Lei, Fang ;

Xiong, Yongxia ;

Wang, Yuqing ;

Zhang, Honghua ;

Liang, Ziyi ;

Li, Junfang ;

Feng, Yiyue ;

Hao, Xiangyong ;

Wang, Zhen .

JOURNAL OF MEDICINAL CHEMISTRY, 2022, 65 (11) :7975-7992

[47] Design, synthesis of novel quinazolin-4-one derivatives and biological evaluation against human MCF-7 breast cancer cell line [J].

Marwa F. Ahmed ;

Amel AA. Hashim .

Research on Chemical Intermediates, 2016, 42 :1777-1789

[48] Design, synthesis and biological evaluation of novel glycosylated diphyllin derivatives as topoisomerase II inhibitors [J].

Shi, Da-Kuo ;

Zhang, Wei ;

Ding, Ning ;

Li, Ming ;

Li, Ying-Xia .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2012, 47 :424-431

[49] Design, synthesis, and biological evaluation of novel benzimidazole derivatives as sphingosine kinase 1 inhibitor [J].

Khairat, Sarah H. M. ;

Omar, Mohamed A. ;

Ragab, Fatma A. F. ;

Roy, Sonam ;

Naqvi, Ahmad A. Turab ;

Abdelsamie, Ahmed S. ;

Hirsch, Anna K. H. ;

Galal, Shadia A. ;

Hassan, Md Imtaiyaz ;

El Diwani, Hoda, I .

ARCHIV DER PHARMAZIE, 2021, 354 (09)

[50] Design, synthesis of novel quinazolin-4-one derivatives and biological evaluation against human MCF-7 breast cancer cell line [J].

Ahmed, Marwa F. ;

Hashim, Amel A. A. .

RESEARCH ON CHEMICAL INTERMEDIATES, 2016, 42 (03) :1777-1789

← 1 2 3 4 5 →