Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives

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, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives
	Liao, Sheng-Rong; Qin, Xiao-Chu; Wang, Zhen; Li, Ding; Xu, Liang; Li, Jin-Sheng; Tu, Zheng-Chao; Liu, Yonghong
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2016
卷号	121 页码:500-509
关键词	2,5-Diketopiperazine derivatives Long alkyl chain Cytotoxic activity Apoptosis Lipophilicity
通讯作者	Liu, YH (reprint author), Chinese Acad Sci, South China Sea Inst Oceanol, Res Ctr Marine Microbes, CAS Key Lab Trop Marine Bioresources & Ecol,Guang, Guangzhou 510301, Guangdong, Peoples R China.
英文摘要	A series of novel N-1-monoallylated 2,5-diketopiperazine derivatives were designed, synthesized, and evaluated as cytotoxic agents against eight cancer cell lines by using CCK8 assay. These derivatives were substituted with methoxyphenyl groups at C-6 position, and various long alkyl side chains at C-3-position of the 2,5-diketopiperazine ring. The cytotoxic results showed that 4-methoxyphenyl group was better than 2-methoxyphenyl group as optimal substitutive group, while 3-methoxyphenyl group was not a suitable one. When the number (n value) of the methylene groups for the long alkyl side chain was 3 (compounds 1c and 3c), the derivatives had the strongest cytotoxicities. Compound 3c substituted with 4-methoxyphenyl group and pentylidene side chain exhibited strong activity (IC50 = 0.36-1.9 mu M) against all cancer cell lines, and could obviously induce apoptosis of cancer cell line U937 at 1.0 mu M after 48 h treatment. (C) 2016 Elsevier Masson SAS. All rights reserved.
学科主题	Pharmacology & Pharmacy
内容类型	期刊论文
源URL	[http://ir.scsio.ac.cn/handle/344004/15279]
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, Sheng-Rong,Qin, Xiao-Chu,Wang, Zhen,et al. Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,121:500-509.
APA	Liao, Sheng-Rong.,Qin, Xiao-Chu.,Wang, Zhen.,Li, Ding.,Xu, Liang.,...&Liu, Yonghong.(2016).Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,121,500-509.
MLA	Liao, Sheng-Rong,et al."Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 121(2016):500-509.