Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors
文献类型：期刊论文
| 作者 | Huang, He2; Jia, Qi1; Ma, Jingui2; Qin, Guangrong2; Chen, Yingyi1; Xi, Yonghua1; Lin, Liping2; Zhu, Weiliang2 ; Ding, Jian2; Jiang, Hualiang2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2009-05 |
| 卷号 | 44期号:5页码:1982-1988 |
| 关键词 | Quercetin Amino acid Src EGFR Inhibitor |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2008.09.051 |
| 文献子类 | Article |
| 英文摘要 | Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC50 values ranging from 3.2 mu M to 9.9 mu M) than against EGFR tyrosine kinase. Molecular docking reveals that both hydrophobic and hydrogen bonding interactions are important to the selectivity. Therefore, this study provides a new promising scaffold for further development of new anticancer drugs targeting Src tyrosine kinase. (C) 2008 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | QUERCETIN ; GROWTH |
| 资助项目 | State Key Program of Basic Research of China[2006BA101B02] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[20872153] ; 863 Hi-Tech Program of China[2006AA020602] ; 863 Hi-Tech Program of China[2006AA02Z336] ; 973 program[2004CB518901] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000265339900020 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279252]  |
| 专题 | 药物化学研究室 药物发现与设计中心 药理学第一研究室 科研与新药推进处 |
| 通讯作者 | Jia, Qi |
| 作者单位 | 1.Shanghai Univ Tradit Chinese Med, Sch Chinese Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, He,Jia, Qi,Ma, Jingui,et al. Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2009,44(5):1982-1988. |
| APA | Huang, He.,Jia, Qi.,Ma, Jingui.,Qin, Guangrong.,Chen, Yingyi.,...&Liu, Hong.(2009).Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,44(5),1982-1988. |
| MLA | Huang, He,et al."Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 44.5(2009):1982-1988. |
入库方式： OAI收割
来源：上海药物研究所
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