中国科学院昆明植物研究所机构知识库
Advanced  
KIB OpenIR  > 中国科学院东亚植物多样性与生物地理学重点实验室  > 期刊论文
题名: Design and synthesis of new 2-arylnaphthyridin-4-ones as potent antitumor agents targeting tumorigenic cell lines
作者: Liu, Chin-Yu1; Cheng, Yung-Yi1; Chang, Ling-Chu1; Huang, Li-Jiau1; Chou, Li-Chen1, 2; Huang, Chi-Hung2; Tsai, Meng-Tung1; Liao, Chih-Chang1; Hsu, Mei-Hua1; Lin, Hui-Yi1; Wu, Tian-Shung3; Wen, Yen-Fang4; Zhao, Yu5, 6; Kuo, Sheng-Chu1, 6; Lee, Kuo-Hsiung6, 7
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期: 2015-01-27
卷号: 90, 页码:775-787
关键词: 2-Arylnaphthyridin-4-ones ; Antitumor agents ; Phosphate prodrug
学科分类: Chemistry, Medicinal
DOI: 10.1016/j.ejmech.2014.11.062
通讯作者: Kuo,SC (reprint author),China Med Univ,Grad Inst Pharmaceut Chem,91 Hsueh Shih Rd,Taichung 40402,Taiwan. ; sckuo@mail.cmu.edu.tw ; khlee@unc.edu
文章类型: Article
英文摘要: To develop new anticancer drug candidates from 2-arylnaphthyridin-4-one (AN), we have designed and synthesized a series of 3'-hydroxy and 6-hydroxy derivatives of AN. The results of cytotoxicity screening indicated that the replacement of the 3'-methoxy moiety on the C-ring phenyl group of AN (6a-e) with 3'-hydroxy (7a-e) made no significant effect on the inhibitory activity against HL-60, Hep3B and NCI-H460 cancer cell lines. On the other hand, replacing the 6-methoxy group on the A-ring of AN (6g-i) with a 6-hydroxy group (7g-i) resulted in reduced inhibitory activity against the above three cancer cell lines. Among the above-mentioned target compounds, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (7a) demonstrated the greatest potency and the best selectivity toward tumorigenic cancer cell lines. In a 7a preliminary mechanism of action study in Hep3B hepatoma cells, 7a showed the effects on microtubules followed by cell cycle arrest and sequentially led to apoptosis.
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: TUBULIN POLYMERIZATION ; BIOLOGICAL EVALUATION ; CYTOTOXICITY ; INHIBITION ; 2-PHENYL-4-QUINOLONES ; MICROTUBULES
收录类别: SCI ; IC
项目资助者: National Science Council of the Republic of China [NSC101-2320-B-039-008] ; National Cancer Institute, NIH [CA177584]
语种: 英语
WOS记录号: WOS:000348951900061
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/20665
Appears in Collections:中国科学院东亚植物多样性与生物地理学重点实验室_期刊论文

Files in This Item: Download All
File Name/ File Size Content Type Version Access License
Liu-2015-Design and synthesis of new 2-arylnap.pdf(1696KB)----开放获取View Download

作者单位: 1.China Med Univ, Grad Inst Pharmaceut Chem, Taichung 40402, Taiwan
2.Hung Kuang Univ, Grad Sch Biotechnol, Taichung 43302, Taiwan
3.Natl Cheng Kung Univ, Dept Chem, Tainan 70101, Taiwan
4.Ind Technol Res Inst, Hsinchu 31040, Taiwan
5.Chinese Acad Sci, Kunming Inst Bot, Kunming 650201, Yunnan, Peoples R China
6.Univ N Carolina, UNC Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA
7.China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung 40447, Taiwan
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Liu, Chin-Yu]'s Articles
[Cheng, Yung-Yi]'s Articles
[Chang, Ling-Chu]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Liu, Chin-Yu]‘s Articles
[Cheng, Yung-Yi]‘s Articles
[Chang, Ling-Chu]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit
文件名: Liu-2015-Design and synthesis of new 2-arylnap.pdf
格式: Adobe PDF
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  中国科学院昆明植物研究所 - Feedback
Powered by CSpace