Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents
Liao, SR; Qin, XC; Li, D; Tu, ZC; Li, JS; Zhou, XF; Wang, JF; Yang, B; Lin, XP; Liu, J; Yang, XW; Liu, YH; yonghongliu@scsio.ac.cn
2014
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号83页码:236-244
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.
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
关键词Solubility 2 Anticancer Agent 5-diketopiperazine Derivative Protective Group
学科领域Pharmacology & Pharmacy
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] ; 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] ; 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] ; 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]
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收录类别sci
资助项目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] ; 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] ; 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] ; 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]
WOS记录号WOS:000340689600020
引用统计
文献类型期刊论文
条目标识符http://ir.scsio.ac.cn/handle/344004/10400
专题中科院海洋生物资源可持续利用重点实验室
通讯作者yonghongliu@scsio.ac.cn
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Liao, SR,Qin, XC,Li, D,et al. Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,83:236-244.
APA Liao, SR.,Qin, XC.,Li, D.,Tu, ZC.,Li, JS.,...&yonghongliu@scsio.ac.cn.(2014).Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,83,236-244.
MLA Liao, SR,et al."Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 83(2014):236-244.
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