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
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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 |
DOI | 10.1016/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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