Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds
文献类型：期刊论文
| 作者 | Wang Fenghua2; Wang Kai1; Shen Jianhua1 ; Chen Kaixian2
|
| 刊名 | Journal of China Pharmaceutical University
 |
| 出版日期 | 2014 |
| 卷号 | 45期号:3页码:286-292 |
| 关键词 | 3-hydroxy-4-quinolone combination synthesis antiproliferative activity structural-activity relationship |
| ISSN号 | 1000-5048 |
| 其他题名 | 3-羟基-4-喹诺酮类化合物的设计、合成及其抗增殖活性 |
| 文献子类 | Article |
| 英文摘要 | A combination of the structural features of dihydromyricetin and quinolone antineoplastic compounds gave rise to 3-hydroxy-4-quinolone motif. Starting from 3,5-dimethoxyaniline,the target compounds were prepared through a reaction cascade,including reductive amination,Friedel-Crafts reaction,microwave assisted ring closure,BBr_3 catalyzed demethylation and Mannich reaction. Sixteen novel compounds were synthesized,and their structures were confirmed by IR,MS and ~1H NMR. The antiproliferative activities of the compounds against A549 and NCI-H 460 cells were tested in MTT assay. Several compounds exhibited moderate antiproliferative activities against both cell lines,of which,compound 11b displayed the most robust inhibition towards NCI-H 460. Preliminary structural-activity relationships indicated that introduction of isopentenyl into the N-1 position of 3-hydroxy-4-quinolone motif would significantly improve the potency of the compounds. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5178677 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269333]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Chen Kaixian |
| 作者单位 | 1.State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. 2.College of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.; |
| 推荐引用方式 GB/T 7714 | Wang Fenghua,Wang Kai,Shen Jianhua,et al. Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds[J]. Journal of China Pharmaceutical University,2014,45(3):286-292. |
| APA | Wang Fenghua,Wang Kai,Shen Jianhua,&Chen Kaixian.(2014).Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds.Journal of China Pharmaceutical University,45(3),286-292. |
| MLA | Wang Fenghua,et al."Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds".Journal of China Pharmaceutical University 45.3(2014):286-292. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。