Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide

doi:10.1016/j.ejmech.2013.11.044

	Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide
	Xu, Hongtao; Tang, Huanyu; Feng, Huijin; Li, Yuanchao
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2014-02-12
卷号	73 页码:46-55
关键词	Triptolide Heterocycle Synthesis Anticancer SKOV-3 PC-3
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2013.11.044
文献子类	Article
英文摘要	Two series of novel C14 heterocycle substituted epi-triptolide derivatives as potential anticancer agents were synthesized and tested for their cytotoxicity against SKOV-3 and PC-3 tumor cell lines. The introduction of C14 beta-aryl heterocycle aminomethyl substituent to the leading compound was found to be an effective modification method to retain the potent anticancer activity. Meanwhile, the series of epitriptolide derivatives (21-40) with C14 alpha-hydroxyl group, still retained the natural product's cytotoxicity. This is apparently challenges the classical structure activity relationship of triptolide that considers the C14 beta-hydroxyl group to be essential for its anticancer activity. (C) 2013 Elsevier Masson SAS. All rights reserved.
资助项目	Shanghai Science and Technology Commission "biomedicine technology support project", China[13431900403] ; National Natural Science Foundation of NFSC, China[81373479]
WOS关键词	TRIPTERYGIUM-WILFORDII ; NATURAL-PRODUCTS ; CELL-DEATH ; APOPTOSIS ; PG490 ; CHEMOTHERAPY ; TRIPDIOLIDE ; ACTIVATION ; CHEMISTRY ; PATHWAY
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000331916500006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277186]
专题	药物化学研究室
通讯作者	Li, Yuanchao
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Xu, Hongtao,Tang, Huanyu,Feng, Huijin,et al. Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,73:46-55.
APA	Xu, Hongtao,Tang, Huanyu,Feng, Huijin,&Li, Yuanchao.(2014).Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,73,46-55.
MLA	Xu, Hongtao,et al."Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 73(2014):46-55.