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题名: Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles
作者: Deng, Xu1, 3; Su, Jia1; Zhao, Yu1; Peng, Li-Yan1; null(李艳)1; Yao, Zhu-Jun2; null(赵勤实)1
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词: Cheliensisin A ; Derivative ; Structure-activity relationship ; Cytotoxicity ; Anticancer
英文摘要: Cheliensisin A is a natural styryl-lactone isolated from Goniothalamus cheliensis Hu in considerably large quantity with putative anticancer activities. However, its poor water solubility and chemical instability have precluded cheliensisin A as a potential drug candidate. To explore the strategy to overcome these problems, 21 novel derivatives of cheliensisin A with different substitutions at C-7 and C-8 positions were designed and synthesized. Inhibition of proliferation against five tumors cell lines indicates that eight new derivatives with embedment of oxazole or oxazoline exhibit improved cytotoxicity on SK-BR-3 and PANC-1, and compounds 2d and 2g show 5-8 folds higher potency than cisplatin. HPLC investigation of representative compounds indicates that oxazole and oxazoline analogs exhibit much improved chemical stability than their natural parent. (C) 2011 Elsevier Masson SAS. All rights reserved.
出版日期: 2011-09-01
卷号: 46, 期号:9, 页码:4238-4244
DOI标识: 10.1016/j.ejmech.2011.06.028
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/151853/3938
Appears in Collections:中国科学院东亚植物多样性与生物地理学重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Bioorgan & Nat Prod Chem, Shanghai 200032, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

Recommended Citation:
Deng, Xu; Su, Jia; Zhao, Yu; Peng, Li-Yan; Li, Yan; Yao, Zhu-Jun; Zhao, Qin-Shi.Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(9):4238-4244
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