中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents

文献类型:期刊论文

作者Wang, Ziwen2; Wu, Meng2; Wang, Yi3; Li, Zheng2; Wang, Lei2; Han, Guifang2; Chen, Fazhong2; Liu, Yuxiu2; Wang, Kailiang2; Zhang, Ao1
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2012-05
卷号51页码:250-258
关键词Phenanthroindolizidine Phenanthroquinolizidine 14-Amino-derivative A549 HL60 Anti-tumor activity
ISSN号0223-5234
DOI10.1016/j.ejmech.2012.02.048
文献子类Article
英文摘要A series of phenanthroindolizidine and phenanthroquinolizidine alkaloids and their 14-amino-derivatives (1-44) were prepared and systematically evaluated for their anti-tumor activities against A549 and HL60 cell lines. The bioassay results showed that most of these alkaloids possess good anti-tumor activities. Especially, compounds 15, 22, 28, 33-36, 40 and 42 displayed low nanomolar or subnanomolar levels of anti-tumor activity. The configuration of (13aS,14S)-14-hydroxyphenanthroindolizidines and (14aR,15R)-15-hydroxyphenanthroquinolizidines was confirmed to be optimal. 14-Amino-phenanthroindolizidines with increased polarity possess good anti-tumor activity, especially for compounds 26 and 28. Most of the phenanthroquinolizidine alkaloids exhibited higher anti-tumor activity than that of phenanthroindolizidine alkaloids. Our present study provides fundamental support for development and optimization of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potential anti-tumor drugs. (C) 2012 Elsevier Masson SAS. All rights reserved.
WOS关键词TYLOPHORINE ANALOG ; QUINOLIZIDINE ALKALOIDS ; PROTEIN-SYNTHESIS ; INDOLIZIDINE ; TYLOCREBRINE ; INHIBITION ; CELLS ; CRYPTOPLEURINE ; PHENANTHRENE ; MODE
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000304291900025
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/278089]  
专题药物化学研究室
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
药理学第一研究室
通讯作者Wang, Qingmin
作者单位1.Chinese Acad Sci, SOMCL, SIMM, Shanghai 201203, Peoples R China;
2.Nankai Univ, State Key Lab Elementoorgan Chem, Res Inst Elementoorgan Chem, Tianjin 300071, Peoples R China;
3.Chinese Acad Sci, Div Antitumor Pharmacol, State Key Lab Drug Res, SIMM, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714
Wang, Ziwen,Wu, Meng,Wang, Yi,et al. Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,51:250-258.
APA Wang, Ziwen.,Wu, Meng.,Wang, Yi.,Li, Zheng.,Wang, Lei.,...&Wang, Qingmin.(2012).Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,51,250-258.
MLA Wang, Ziwen,et al."Synthesis and SAR studies of phenanthroindolizidine and phenanthroquinolizidine alkaloids as potent anti-tumor agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 51(2012):250-258.

入库方式: OAI收割

来源:上海药物研究所

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