The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors
文献类型：期刊论文
| 作者 | Zhang, Xuan2 ; Su, Mingbo1; Chen, Yi3; Li, Jia3; Lu, Wei2
|
| 刊名 | MOLECULES
 |
| 出版日期 | 2013-06 |
| 卷号 | 18期号:6页码:6491-6503 |
| 关键词 | receptor tyrosine kinases histone deacetylase antitumor synergistic effect dual inhibitor |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules18066491 |
| 文献子类 | Article |
| 英文摘要 | Over the years, the development of targeted medicines has made significant achievements. As a typical example, receptor tyrosine kinases (RTK) inhibitors have become important chemotherapy drugs for a variety of cancers. However, the effectiveness of these agents is always hindered by poor response rates and acquired drug resistance. In order to overcome these limitations, several dual-targeted inhibitors with quinazoline core were designed and synthesized. Though these compounds can simultaneously inhibit histone deacetylases (HDAC) as well as RTK, the structure-activity relationship (SAR) is still not clear enough. To further explore this type of dual-targeted inhibitors, a new class of quinazoline derivatives were designed and synthesized. Their activity evaluations include in vitro inhibitory activity of HDAC, epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). The SAR study indicated that the introduction of polar group such as hydroxamate on the 4-position of the quinazoline core is more likely to provide a potent HDACi/HER2i hybrid rather than HDACi/EGFRi molecule. |
| WOS关键词 | HISTONE DEACETYLASE INHIBITORS ; GROWTH-FACTOR RECEPTOR ; T-CELL LYMPHOMA ; POTENT INHIBITORS ; CANCER-THERAPY ; LUNG-CANCER ; IN-VIVO ; SERIES ; PERSPECTIVES ; VORINOSTAT |
| 资助项目 | State Key Laboratory of Drug Research[SIMM1203KF-10] ; National Natural Science Foundation of China[81172936] ; National Natural Science Foundation of China[21102046] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000320770800021 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277595]  |
| 专题 | 国家新药筛选中心 中国科学院上海药物研究所 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 药物安全性评价中心 |
| 通讯作者 | Lu, Wei |
| 作者单位 | 1.E China Normal Univ, Sch Life Sci, Shanghai 200062, Peoples R China; 2.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Xuan,Su, Mingbo,Chen, Yi,et al. The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors[J]. MOLECULES,2013,18(6):6491-6503. |
| APA | Zhang, Xuan,Su, Mingbo,Chen, Yi,Li, Jia,&Lu, Wei.(2013).The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors.MOLECULES,18(6),6491-6503. |
| MLA | Zhang, Xuan,et al."The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors".MOLECULES 18.6(2013):6491-6503. |
入库方式： OAI收割
来源：上海药物研究所
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