Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues

doi:10.1016/j.ejmech.2008.04.004

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues
	Lu, Hong-Fu 3; Sun, Xun 3; Xu, Liang 1; Lou, Li-Guang2 ; Lin, Guo-Qiang 1,3
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2009-02
卷号	44 期号:2 页码:482-491
关键词	Docetaxel Fluorinated docetaxel analogues Cytotoxicity
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2008.04.004
文献子类	Article
英文摘要	A series of novel fluorinated docetaxel analogues have been synthesized and evaluated in vitro and in vivo. Incorporated one, two or three fluorine atom(s) either at both meta position on C-2 benzolate and 3'-N-tert-butyloxyl group or only at 3-N-tert-butyloxyl group has resulted in potent analogues which have comparable or superior in vitro and in vivo cytotoxicity to docetaxel. Among them, compounds 14d and 14e have displayed more potent cytotoxicity than docetaxel both in human cancer cell line SK-OV-3 in vitro and in human non-small cell lung cancer A549 xenografts in vivo. Preliminary data show that compound 14a has reduced acute animal toxicity in mice compared with docetaxel. (C) 2008 Elsevier Masson SAS. All rights reserved.
资助项目	National Natural Science Foundation of China[20772017] ; Shanghai Municipal Committee of Science and Technology[07DZ19713]
WOS关键词	CONTAINING TAXOIDS ; HEMISYNTHESIS ; METABOLISM
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:000264407800004
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279330]
专题	药理学第一研究室
通讯作者	Sun, Xun
作者单位	1.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Fudan Univ, Sch Pharm, Dept Chem Nat Drugs, Shanghai 200032, Peoples R China;
推荐引用方式 GB/T 7714	Lu, Hong-Fu,Sun, Xun,Xu, Liang,et al. Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2009,44(2):482-491.
APA	Lu, Hong-Fu,Sun, Xun,Xu, Liang,Lou, Li-Guang,&Lin, Guo-Qiang.(2009).Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,44(2),482-491.
MLA	Lu, Hong-Fu,et al."Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 44.2(2009):482-491.