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题名: Synthesis and cytotoxicity of some new eriocalyxin B derivatives
作者: Zhao, Yu; Niu, Xue-Mei; Qian, Li-Ping; Liu, Ze-Yuan; null(赵勤实); null(孙汉董)
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词: eriocalyxin B ; synthesis ; cytotoxicity ; SAR
英文摘要: 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.
出版日期: 2007-04-01
卷号: 42, 期号:4, 页码:494-502
DOI标识: 10.1016/j.ejmech.2006.11.004
语种: 英语
ISSN号: 0223-5234
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/2093
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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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

Recommended Citation:
Zhao, Y; Niu, XM; Qian, LP; Liu, ZY; Zhao, QS; Sun, HD.Synthesis and cytotoxicity of some new eriocalyxin B derivatives,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2007,42(4):494-502
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