Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase
文献类型：期刊论文
| 作者 | Huang, He2; Ma, Jingui1; Shi, Jianmei2; Meng, Linghua1 ; Jiang, Hualiang2; Ding, Jian1; Liu, Hong2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010-07-01 |
| 卷号 | 18期号:13页码:4615-4624 |
| 关键词 | c-Src tyrosine kinase Inhibitor Purine derivative Focused library |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2010.05.032 |
| 文献子类 | Article |
| 英文摘要 | We report here the discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase by adopting a strategy integrating focused combinatorial library design, virtual screening, chemical synthesis, and bioassay. Thirty two compounds were selected and synthesized. All compounds showed potent inhibitory activity against c-Src kinase with IC50 values ranging from 3.14 mu M to 0.02 mu M. Compound 5i was identified as one of the most potent agent with an IC50 120 times lower than those of the hits. The high hit rate (100%) and the potency of the new Src kinase inhibitors demonstrated the efficiency of the strategy for the focused library design and virtual screening. The novel active chemical entities reported here should be good leads for further development of purine-based anticancer drugs targeting Src tyrosine kinase. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BIOLOGICAL EVALUATION ; FAMILY KINASES ; STRUCTURAL BASIS ; BREAST-CANCER ; TARGETING SRC ; DESIGN ; METASTASES ; BMS-354825 ; GROWTH ; AGENTS |
| 资助项目 | State Key Program of Basic Research of China[2002CB512802] ; National Natural Science Foundation of China[20372069] ; National Natural Science Foundation of China[29725203] ; 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[2006AA020402] ; National S&T Major Projects[2009ZX09301-001] ; National S&T Major Projects[2009ZX09501-001] ; National S&T Major Projects[2009ZX09501-010] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000279011000003 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278847]  |
| 专题 | 药理学第一研究室 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 药物发现与设计中心 药物化学研究室 |
| 通讯作者 | Meng, Linghua |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, He,Ma, Jingui,Shi, Jianmei,et al. Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2010,18(13):4615-4624. |
| APA | Huang, He.,Ma, Jingui.,Shi, Jianmei.,Meng, Linghua.,Jiang, Hualiang.,...&Liu, Hong.(2010).Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.BIOORGANIC & MEDICINAL CHEMISTRY,18(13),4615-4624. |
| MLA | Huang, He,et al."Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase".BIOORGANIC & MEDICINAL CHEMISTRY 18.13(2010):4615-4624. |
入库方式： OAI收割
来源：上海药物研究所
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