Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents

CORC > 南海海洋研究所 > 中国科学院南海海洋研究所 > 中科院海洋生物资源可持续利用重点实验室

	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
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2014
卷号	83 页码:236-244
关键词	2 Solubility Anticancer agent Protective group 5-Diketopiperazine derivative
ISSN号	0223-5234
通讯作者	yonghongliu@scsio.ac.cn
中文摘要	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.
学科主题	Pharmacology & Pharmacy
收录类别	SCI
资助信息	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]
原文出处	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000340689600020
公开日期	2014-12-11
内容类型	期刊论文
源URL	[http://ir.scsio.ac.cn/handle/344004/10400]
专题	南海海洋研究所_中科院海洋生物资源可持续利用重点实验室
推荐引用方式 GB/T 7714	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.,...&Liu, YH.(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.