Synthesis and cytotoxicity of some new eriocalyxin B derivatives

doi:10.1016/j.ejmech.2006.11.004

	Synthesis and cytotoxicity of some new eriocalyxin B derivatives
	Zhao, Yu ; Niu, Xue-Mei ; Qian, Li-Ping ; Liu, Ze-Yuan ; Zhao, Qin-Shi; Sun, Han-Dong
	2007-04-01
发表期刊	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0223-5234
卷号	42 期号:4 页码:494-502
摘要	Eriocalyxin B (1) was regarded as the promising candidate for new anticancer agent because of its potent activity and novel mechanism of action. Systematic modifications of 1 were done, and nineteen derivatives were synthesized and their cytotoxicities against five tumor cell lines were evaluated. The structure-activity relationship (SAR) of 1 confirmed that the alpha,beta-unsaturated ketone moieties in ring A and D are the leading active sites; the 7,20-epoxy moiety, OH-6 and OH-7 play an important role in keeping the cytotoxicity. The 6,7-seco derivative 19 had remarkable activity while derivative 20 oxidized from 19 was completely inactive, which suggested that the carboxyl group could destroy the cytoxicity of 20 despite the presence of alpha,beta-unsaturated ketone moiety. (c) 2006 Elsevier Masson SAS. All rights reserved.
关键词	Eriocalyxin b Synthesis Cytotoxicity Sar
学科领域	Chemistry ; Medicinal
DOI	10.1016/j.ejmech.2006.11.004
收录类别	SCI ; IC
语种	英语
WOS记录号	WOS:000246268500009
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/2093
专题	植物化学与西部植物资源持续利用国家重点实验室
作者单位	1.Acad Mil Med Sci, Affiliated Hosp, Dept Clin Pharmacol, Beijing 100039, Peoples R China 2.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China 3.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Yunnan, Peoples R China
推荐引用方式 GB/T 7714	Zhao, Yu,Niu, Xue-Mei,Qian, Li-Ping,et al. Synthesis and cytotoxicity of some new eriocalyxin B derivatives[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2007,42(4):494-502.
APA	Zhao, Yu,Niu, Xue-Mei,Qian, Li-Ping,Liu, Ze-Yuan,Zhao, Qin-Shi,&Sun, Han-Dong.(2007).Synthesis and cytotoxicity of some new eriocalyxin B derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,42(4),494-502.
MLA	Zhao, Yu,et al."Synthesis and cytotoxicity of some new eriocalyxin B derivatives".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 42.4(2007):494-502.

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