Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles

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	Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles
	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)
刊名	Eur. J. Med. Chem.
	2011
卷号	46 期号:9 页码:4238-4244
ISSN号	0223-5234
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
通讯作者	姚祝军 ; 赵勤实
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.
学科主题	生命有机化学
收录类别	SCI
原文出处	http://dx.doi.org/10.1016/j.ejmech.2011.06.028
语种	英语
WOS记录号	WOS:000295237400074
公开日期	2013-02-26
内容类型	期刊论文
源URL	[http://202.127.28.38/handle/331003/21159]
专题	上海有机化学研究所_生命有机化学国家重点实验室
推荐引用方式 GB/T 7714	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.
APA	邓旭.,苏佳.,赵昱.,彭丽艳.,李艳.,...&赵勤实.(2011).Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles.Eur. J. Med. Chem.,46(9),4238-4244.
MLA	邓旭,et al."Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles".Eur. J. Med. Chem. 46.9(2011):4238-4244.