Design and Synthesis of a Series of Novel Bisquinazoline Glycosides as Epidermal Growth Factor Receptor Inhibitors
文献类型：期刊论文
| 作者 | Chen, Shaopeng1; Zhang, Xiaowei2; Wang, Junlei1; Wan, Shengbiao1; Geng, Meiyu2 ; Jiang, Tao1
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| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
 |
| 出版日期 | 2011-12 |
| 卷号 | 78期号:6页码:1006-1013 |
| 关键词 | epidermal growth factor receptor inhibition glycoside quinazoline |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/j.1747-0285.2011.01209.x |
| 文献子类 | Article |
| 英文摘要 | A new series of potential epidermal growth factor receptor inhibitors possessing bisquinazoline and saccharide moieties were designed and synthesized. The biological results demonstrated that the synthetic derivatives significantly inhibited epidermal growth factor receptor enzymatic activity in vitro. Of them, compound 14b showed the highest inhibitory rate toward epidermal growth factor receptor protein tyrosine kinase (81.36%) at a concentration of 1 mu m. Further molecular simulation predicted that 14b offered its saccharide moieties hydrogen bonding to ATP-binding pocket. |
| WOS关键词 | TYROSINE KINASE INHIBITORS ; CANCER-THERAPY ; EGF-RECEPTOR |
| 资助项目 | CMST[2008DFA31040] ; Natural Science Foundation of China[30725046] ; Program for Changjiang Scholars and Innovative Research Team in University[IRT0944] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000297095000013 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278319]  |
| 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 |
| 通讯作者 | Jiang, Tao |
| 作者单位 | 1.Ocean Univ China, Sch Med & Pharm, Key Lab Marine Drugs, Minist Educ China, Qingdao 266003, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Shaopeng,Zhang, Xiaowei,Wang, Junlei,et al. Design and Synthesis of a Series of Novel Bisquinazoline Glycosides as Epidermal Growth Factor Receptor Inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2011,78(6):1006-1013. |
| APA | Chen, Shaopeng,Zhang, Xiaowei,Wang, Junlei,Wan, Shengbiao,Geng, Meiyu,&Jiang, Tao.(2011).Design and Synthesis of a Series of Novel Bisquinazoline Glycosides as Epidermal Growth Factor Receptor Inhibitors.CHEMICAL BIOLOGY & DRUG DESIGN,78(6),1006-1013. |
| MLA | Chen, Shaopeng,et al."Design and Synthesis of a Series of Novel Bisquinazoline Glycosides as Epidermal Growth Factor Receptor Inhibitors".CHEMICAL BIOLOGY & DRUG DESIGN 78.6(2011):1006-1013. |
入库方式： OAI收割
来源：上海药物研究所
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