Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives

doi:10.1016/j.fitote.2016.07.002

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	Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives
	Chen, Hu 1; Lei, Min2 ; Ma, Biao 2; Liu, Miao 2; Guo, Dean2 ; Liu, Xuan 2; Hu, Lihong 1,2
刊名	FITOTERAPIA
	2016-09
卷号	113 页码:85-90
关键词	Oleandrin Antitumor agent Natural product Cytotoxicity Structure-activity relationships (SARs)
ISSN号	0367-326X
DOI	10.1016/j.fitote.2016.07.002
文献子类	Article
英文摘要	A series of C4'-substituted oleandrin analogues were designed, synthesized and evaluated for their cytotoxicity towards human cervical carcinoma cell line (HeLa). The structure-activity relationships (SARs) of these compounds were summarized in this paper, and 4'-alpha-amino-4'-dehydroxyloleandrin 4a (IC50 = 21.7 nM) and 4'-beta-amino-4'-dehydroxyloleandrin 4b (IC50 = 10.9 nM) exhibited stronger cytotoxicity compared with oleandrin (IC50 = 33.3 nM). Furthermore, the cytotoxicity of these two compounds towards another five human cancer cell lines (NCI-H266, A549, Jurkat, HL-60 and PC-3) was also evaluated and the IC50 values of beta-amino derivative 4b were approximately 2-3 folds lower than that of oleandrin. (C) 2016 Published by Elsevier B.V.
资助项目	Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2013ZX09508104] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09301306-003] ; Shanghai Science & Technology Support Program[13431900401]
WOS关键词	MADAGASCAR RAIN-FOREST ; CARDIAC-GLYCOSIDES ; CARDENOLIDE GLYCOSIDES ; CELL-DEATH ; POTENTIATES APOPTOSIS ; NERIUM-OLEANDER ; CANCER-CELLS ; SOLID TUMORS ; ACTIVATION ; EXPRESSION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000383301200012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275912]
专题	上海中药现代化研究中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Lei, Min; Liu, Xuan; Hu, Lihong
作者单位	1.East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Chen, Hu,Lei, Min,Ma, Biao,et al. Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives[J]. FITOTERAPIA,2016,113:85-90.
APA	Chen, Hu.,Lei, Min.,Ma, Biao.,Liu, Miao.,Guo, Dean.,...&Hu, Lihong.(2016).Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives.FITOTERAPIA,113,85-90.
MLA	Chen, Hu,et al."Synthesis and cytotoxicity evaluation of 4 '-amino-4 '-dehydroxyloleandrin derivatives".FITOTERAPIA 113(2016):85-90.