Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin

doi:10.1016/j.steroids.2020.108749

	Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin
	Zhou, Yang 1,2; Hou, Jinjun 1,2; Long, Huali 1,2; Zhang, Zijia 1,2; Lei, Min 1,2; Wu, Wanying 1,2
刊名	STEROIDS
	2020-12-01
卷号	164 页码:11
关键词	Cardiac glycosides Cinobufagin Natural product Cytotoxicity Antiproliferative activities
ISSN号	0039-128X
DOI	10.1016/j.steroids.2020.108749
通讯作者	Lei, Min(mlei@simm.ac.cn) ; Wu, Wanying(wanyingwu@simm.ac.cn)
英文摘要	A series of cinobufagin-3-yl nitrogen-containing-carbamate derivatives were designed, synthesized, and evalu-ated for their proliferation inhibition activities. The structure-activity relationships suggested that the substituents at C-16 was a crucial factor for the potency and that follows this trends: acetic ester >> benzoic ester approximate to hydroxy > carbamate. Compounds 3f, 3g, 3h, and 3i exhibited significant in vitro antiproliferative activities against the eight tested tumor cell lines, with IC50 values ranging from 8.1 to 237.4 nM. Furthermore, 3g tartrate (3g-TA) significantly inhibited tumor growth by 64.5%, 83.9%, and 93.0% at a doses of 4, 6, 8 mg/kg/qod by ip, respectively.
资助项目	Special Fund for Strategic Pilot Technology Chinese Academy of Sciences[XDA12020379] ; National Natural Science Foundation of China[81973455] ; National Key R&D Program of China[2018YFC1707900]
WOS关键词	CARDIAC-GLYCOSIDES ; CARDENOLIDE GLYCOSIDES ; BUFADIENOLIDES ; CYTOTOXICITY
WOS研究方向	Biochemistry & Molecular Biology ; Endocrinology & Metabolism
语种	英语
出版者	ELSEVIER SCIENCE INC
WOS记录号	WOS:000592420700009
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/296217]
专题	中国科学院上海药物研究所
通讯作者	Lei, Min; Wu, Wanying
作者单位	1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai Inst Mat Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhou, Yang,Hou, Jinjun,Long, Huali,et al. Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin[J]. STEROIDS,2020,164:11.
APA	Zhou, Yang,Hou, Jinjun,Long, Huali,Zhang, Zijia,Lei, Min,&Wu, Wanying.(2020).Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin.STEROIDS,164,11.
MLA	Zhou, Yang,et al."Design, synthesis and anti-tumor activities of carbamate derivatives of cinobufagin".STEROIDS 164(2020):11.