中国科学院南海海洋研究所机构知识库
Advanced  
SCSIO OpenIR  > 中科院海洋生物资源可持续利用重点实验室  > 期刊论文
学科主题: Pharmacology & Pharmacy
题名: Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents
作者: Liao, SR ; Qin, XC ; Li, D ; Tu, ZC ; Li, JS ; Zhou, XF ; Wang, JF ; Yang, B ; Lin, XP ; Liu, J ; Yang, XW ; Liu, YH
通讯作者: yonghongliu@scsio.ac.cn
关键词: 2,5-Diketopiperazine derivative ; Solubility ; Anticancer agent ; Protective group
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2014
卷: 83, 页:236-244
收录类别: sci
部门归属: [Liao, Shengrong ; Li, Jinsheng ; Zhou, Xuefeng ; Wang, Junfeng ; Yang, Bin ; Lin, Xiuping ; Liu, Juan ; Yang, Xianwen ; Liu, Yonghong] Chinese Acad Sci, CAS Key Lab Trop Marine Bioresources & Ecol, Guangdong Key Lab Marine Mat Med, South China Sea Inst Oceanol,RNAM Ctr Marine Micr, Guangzhou 510301, Guangdong, Peoples R China ; [Qin, Xiaochu ; Tu, Zhengchao] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Lab Mol Engn, Guangzhou 510530, Guangdong, Peoples R China ; [Qin, Xiaochu ; Tu, Zhengchao] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Lab Nat Prod Synth, Guangzhou 510530, Guangdong, Peoples R China ; [Li, Ding] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
项目归属: LMB
资助者: National Key Basic Research Program of China (973)'s Project [2010CB833800, 2011CB915503]; National High Technology Research and Development Program (863 Program) [2012AA092104]; National Natural Science Foundation of China [31270402, 21172230, 30973679, 41176148, 21002110]; Guangdong Province-CAS Joint Research Program [2011B090300023, 2012B091100264]; Guangdong Marine Economic Development and Innovation of Regional Demonstration Project [GD2012-D01-001, GD2012D01-002]
摘要: Non-protected 2,5-diketopiperazine derivatives have poor solubility thus with negative impact on their bioavailability. In the present study, twenty-one novel soluble mono-protected, and three non-protected 2,5-diketopiperazine derivatives were designed and synthesized. Their anticancer activity to ten cell lines were evaluated by using CCK8 assay, and the results showed that about half of the mono-protected derivatives had broad-spectrum anticancer activity. Among allyl-protected derivatives, compound 4m had strong activity to all the cell lines (IC50 = 0.5-4.5 mu M), especially to the cancer cell lines U937 (IC50 = 0.5 mu M) and K562 (IC50 = 0.9 mu M). Compound 4m could become a lead compound for further development for anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
原文出处: 查看原文
WOS记录号: WOS:000340689600020
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.scsio.ac.cn/handle/344004/10400
Appears in Collections:中科院海洋生物资源可持续利用重点实验室_期刊论文

Files in This Item: Download All
File Name/ File Size Content Type Version Access License
1-s2.0-S0223523414005492-main.pdf(952KB)----开放获取View Download

Recommended Citation:
Liao, SR; Qin, XC; Li, D; Tu, ZC; Li, JS; Zhou, XF; Wang, JF; Yang, B; Lin, XP; Liu, J; Yang, XW; Liu, YH.Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,83():236-244
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Liao, SR]'s Articles
[Qin, XC]'s Articles
[Li, D]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Liao, SR]‘s Articles
[Qin, XC]‘s Articles
[Li, D]‘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: 1-s2.0-S0223523414005492-main.pdf
格式: Adobe PDF
此文件暂不支持浏览
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  中国科学院南海海洋研究所 - Feedback
Powered by CSpace