Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives

doi:10.1021/np900157t

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	Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives
	Shao, Yong 1; Zhang, Han-Kun 1; Ding, Hong2 ; Quan, Hai-Tian2 ; Lou, Li-Guang2 ; Hu, Li-Hong 1
刊名	JOURNAL OF NATURAL PRODUCTS
	2009-06
卷号	72 期号:6 页码:1170-1177
ISSN号	0163-3864
DOI	10.1021/np900157t
文献子类	Article
英文摘要	A series of 3-demethoxycarbonyl-3-amide methyl anhydrovinblastine derivatives (5b-24b) was designed, synthesized, and evaluated for their proliferation inhibition activities against two tumor cell lines (A549 and HeLa). Most of the amide anhydrovinblastine derivatives exhibited potent cytotoxicity, with the size of the introduced substituents being the foremost factor in determining the resultant cytotoxic activity. Test results in vivo against sarcoma 180 of three potent compounds (6b, 12b, and 24b) indicated that the introduction of an amide group at the 22-position of anhydrovinblastine (1e) improved both potency and toxicity.
资助项目	Chinese National High-tech RD Program[2007AA02Z147] ; Chinese National High-tech RD Program[2006AA020602] ; Natural Science Foundation of China[90713046] ; Natural Science Foundation of China[30772638] ; CAS Foundation[KSCX2-YW-R-18]
WOS关键词	DIMERIC CATHARANTHUS ALKALOIDS ; AMINO-ACID DERIVATIVES ; VINCA ALKALOIDS ; VINDESINE ; AGENTS ; DISCOVERY ; ANALOGS ; PART
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000267432600035
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279229]
专题	上海中药现代化研究中心
通讯作者	Hu, Li-Hong
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Mol Pharmacol, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Shao, Yong,Zhang, Han-Kun,Ding, Hong,et al. Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives[J]. JOURNAL OF NATURAL PRODUCTS,2009,72(6):1170-1177.
APA	Shao, Yong,Zhang, Han-Kun,Ding, Hong,Quan, Hai-Tian,Lou, Li-Guang,&Hu, Li-Hong.(2009).Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives.JOURNAL OF NATURAL PRODUCTS,72(6),1170-1177.
MLA	Shao, Yong,et al."Synthesis and Structure-Activity Relationship Studies of Cytotoxic Anhydrovinblastine Amide Derivatives".JOURNAL OF NATURAL PRODUCTS 72.6(2009):1170-1177.