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

[21] Design, synthesis, and biological evaluation of novel atorvastatin derivatives
Najafi, Shiva
Moshtaghie, Ali Asghar
Hassanzadeh, Farshid
Nayeri, Hashem
Jafari, Elham
JOURNAL OF MOLECULAR STRUCTURE, 2023, 1282
[22] Design, synthesis and biological evaluation of novel asperphenamate derivatives
Liu, Qingyin
Li, Wei
Sheng, Lei
Zou, Chunyang
Sun, Hongxin
Zhang, Chunfeng
Liu, Yang
Shi, Jiyue
Ma, Enlong
Yuan, Lei
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 110 : 76 - 86
[23] Design, Synthesis and Biological Evaluation of Amide Derivatives of Thiazolo[5,4-d]Pyrimidines as Cytotoxicity Agents for Human Cancer Cell Lines
Balaraju, V.
Laxminarayana, E.
Kalyani, S.
PHARMACEUTICAL CHEMISTRY JOURNAL, 2023, 57 (08) : 1241 - 1250
[24] Design, Synthesis and Biological Evaluation of Amide Derivatives of Thiazolo[5,4-d]Pyrimidines as Cytotoxicity Agents for Human Cancer Cell Lines
V. Balaraju
E. Laxminarayana
S. Kalyani
Pharmaceutical Chemistry Journal, 2023, 57 : 1241 - 1250
[25] Pyrimidooxadiazine and triazolopyrimidooxadiazine derivatives: Synthesis and cytotoxic evaluation in human cancer cell lines
Mousavi, Seyed-Hadi
Atapour-Mashhad, Hoda
Bakavoli, Mehdi
Shiri, Ali
Akbarzadeh, Marzieh
Tayarani-Najaran, Zahra
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY, 2015, 41 (02) : 201 - 208
[26] Pyrimidooxadiazine and triazolopyrimidooxadiazine derivatives: Synthesis and cytotoxic evaluation in human cancer cell lines
Seyed-Hadi Mousavi
Hoda Atapour-Mashhad
Mehdi Bakavoli
Ali Shiri
Marzieh Akbarzadeh
Zahra Tayarani-Najaran
Russian Journal of Bioorganic Chemistry, 2015, 41 : 201 - 208
[27] Synthesis and evaluation of coumarin derivatives against human lung cancer cell lines
Weng, K. -G.
Yuan, Y. -L.
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH, 2017, 50 (11)
[28] Design, synthesis, crystal structure, biological evaluation and molecular docking studies of carbazole-arylpiperazine derivatives
Xu, Wei
Huang, Junjun
Shao, Binhao
Xu, Xingjie
Jiang, Renwang
Yuan, Mu
BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 24 (21) : 5565 - 5572
[29] Design, synthesis, and biological evaluation of C-8 modified curcumol derivatives against colorectal cancer cell lines
Nong, Bin-Lu
Meng, Xiang-Wei
Wei, Ying-Ying
Zhao, Hua-Jun
Zhang, Xing-Xian
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH, 2023, 25 (03) : 287 - 300
[30] Induction of Apoptosis in Hepatocellular Carcinoma Cell Lines by Novel Indolylacrylamide Derivatives: Synthesis and Biological Evaluation
Hawash, Mohammed
Kahraman, Deniz Cansen
Cetin-Atalay, Rengul
Baytas, Sultan Nacak
CHEMISTRY & BIODIVERSITY, 2021, 18 (05)

← 1 2 3 4 5 →