Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity

doi:10.1016/j.ejmech.2017.09.016

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	Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity
	Liu, Xian-xuan 1; Yang, Yan-ting 1; Wang, Xiao 1; Wang, Kai-yi 1; Liu, Jia-qi 1; Lei, Lei 1,3,4; Luo, Xiao-min2 ; Zhai, Rong 1; Fu, Feng-hua 1; Wang, Hong-bo 1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2017-12-01
卷号	141 页码:427-439
关键词	alpha-Hederagenin derivatives Synthesis Apoptosis Cancer
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2017.09.016
文献子类	Article
英文摘要	In an attempt to arrive at a more potent cytotoxic agent than the parent compound a-hederagenin (H), 24 alpha-hederagenin derivatives (5-8,11-24, 27-28, 31-32, and 35-36) were synthesized in a concise and efficient strategy and screened for in vitro cytotoxicity against the human cancer cell lines MKN45 and KB. Among these compounds, the polyamine derivative 15 exhibited more potency than the parent compound with IC50 values in the range of 4.22 AM-8.05 mu M. Compound 15 increased Baxibc1-2 ratio that disrupted the mitochondrial potential and induced apoptosis. Therefore, the present studies highlight the importance of polyamine derivatives of alpha-hederagenin in the discovery and development of novel anticancer agents. (C) 2017 Elsevier Masson SAS. All rights reserved.
资助项目	State Key Laboratory of Drug Research[SIMM1705KF-07] ; Taishan Scholar Project[00000000] ; Graduate Innovation Foundation of Yantai University, GIFYTU[YDZD1717]
WOS关键词	CYTOTOXIC ACTIVITY ; APOPTOSIS ; ACID ; CARCINOGENESIS ; MITOCHONDRIA
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:000417962900036
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272364]
专题	新药研究国家重点实验室中科院受体结构与功能重点实验室
通讯作者	Wang, Hong-bo; Bi, Yi
作者单位	1.Yantai Univ, Key Lab Mol Pharmacol & Drug Evaluat, Collaborat Innovat Ctr Adv Drug Delivery Syst & B, Sch Pharm,Minist Educ, Yantai 264005, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Peking Union Med Coll, Beijing 100050, Peoples R China; 4.Chinese Acad Med Sci, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China;
推荐引用方式 GB/T 7714	Liu, Xian-xuan,Yang, Yan-ting,Wang, Xiao,et al. Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2017,141:427-439.
APA	Liu, Xian-xuan.,Yang, Yan-ting.,Wang, Xiao.,Wang, Kai-yi.,Liu, Jia-qi.,...&Bi, Yi.(2017).Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,141,427-439.
MLA	Liu, Xian-xuan,et al."Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 141(2017):427-439.