Design, synthesis and biological evaluation of novel alpha-hederagenin derivatives with anticancer activity
文献类型：期刊论文
| 作者 | Liu, Xian-xuan1; Yang, Yan-ting1; Wang, Xiao1; Wang, Kai-yi1; Liu, Jia-qi1; Lei, Lei1,3,4; Luo, Xiao-min2 ; Zhai, Rong1; Fu, Feng-hua1; Wang, Hong-bo1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 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. |
| WOS关键词 | CYTOTOXIC ACTIVITY ; APOPTOSIS ; ACID ; CARCINOGENESIS ; MITOCHONDRIA |
| 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研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000417962900036 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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