Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins

doi:10.1016/j.bmc.2004.06.003

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	Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins
	He, XG ; Lu, W ; Jiang, XQ ; Cai, JC ; Zhang, XW ; Ding, J
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2004-08-01
卷号	12 期号:15 页码:4003-4008
关键词	camptothecin 10-hydroxycamptothecin carbonate anti-tumor
ISSN号	0968-0896
DOI	10.1016/j.bmc.2004.06.003
文献子类	Article
英文摘要	In an effort to improve the stability of labile lactone ring of camptothecins, the his and mono-alkyl carbonate prodrugs of 10-hydroxycamptothecins were synthesized and their chemical and enzymatical stability as well as antitumor activity were studied. The in vitro evaluation of the stability of these carbonates indicates that the 10,20-biscarbonates are firstly hydrolyzed to afford the stable 20-monocarbonates. And the 10-carbonates are not stable in human plasma, mouse plasma and pH 7.4 phosphate buffer, while the 20-carbonates are relatively stable in the three media and can be readily cleaved by porcine liver esterase. The overall toxicity of the tested carbonate against mice bearing S 180 sarcoma is much lower when compared with the parent compound, and the antitumor activity is maintained. (C) 2004 Elsevier Ltd. All rights reserved.
WOS关键词	ANTITUMOR-ACTIVITY ; CAMPTOTHECIN ; DERIVATIVES ; CANCER
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000222886700006
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274039]
专题	药理学第一研究室
通讯作者	Lu, W
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China 2.Nanjing Univ, Jiangsu Prov Lab Nanotechnol, Nanjing 210093, Peoples R China
推荐引用方式 GB/T 7714	He, XG,Lu, W,Jiang, XQ,et al. Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2004,12(15):4003-4008.
APA	He, XG,Lu, W,Jiang, XQ,Cai, JC,Zhang, XW,&Ding, J.(2004).Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins.BIOORGANIC & MEDICINAL CHEMISTRY,12(15),4003-4008.
MLA	He, XG,et al."Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins".BIOORGANIC & MEDICINAL CHEMISTRY 12.15(2004):4003-4008.