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学科主题: 生命有机化学
题名: Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles
其他题名: 通过嵌入小杂环发展景洪哥纳香甲素的新型构象约束的细胞毒素衍生物
作者: Deng X(邓旭) ; Su J(苏佳) ; Zhao Y(赵昱) ; Peng LY(彭丽艳) ; Li Y(李艳) ; Yao ZJ(姚祝军) ; Zhao QS(赵勤实)
通讯作者: 姚祝军 ; 赵勤实
刊名: Eur. J. Med. Chem.
发表日期: 2011
卷: 46, 期:9, 页:4238-4244
收录类别: SCI
部门归属: 中科院昆明植物研究所; 中科院上海有机化学研究所; 中科院研究生院
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.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000295237400074
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/21159
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
Deng X,Su J,Zhao Y,et al. Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles[J]. Eur. J. Med. Chem.,2011,46(9):4238-4244.
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