Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs)
文献类型：期刊论文
| 作者 | Wang, Xin1 ; Chen, Zhuo1,2; Tong, Linjiang2; Tan, Shaoying1; Zhou, Wei1; Peng, Ting2; Han, Kun2; Ding, Jian2; Xie, Hua2; Xu, Yufang1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2013-07 |
| 卷号 | 65页码:477-486 |
| 关键词 | Angiogenesis Multitarget Naphthalimide Topoisomerase II Tyrosine kinase |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2013.05.002 |
| 文献子类 | Article |
| 英文摘要 | Novel naphthalimide derivatives were designed and synthesized to modulate both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs). Most target compounds exhibited effective and selective antiproliferative activities against three cancer cell lines by inhibiting topo II. The IC50 values ranged from 1.5 to 19.1 mu M. Moreover, compounds 8d and 12d moderately inhibited various angiogenesis-related RTKs, including FGFR1, VEGFR2 and PDGFR alpha. The representative compound 8d was then proved to possess antiangiogenic activity, which was evidenced by the inhibition of migration and tube formation activities of HMEC-1 cells. To our knowledge, it is the first time naphthalimides were identified as tyrosine kinases inhibitors (TKIs) besides their conventional cytotoxicity. (C) 2013 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | ANTITUMOR AGENTS ; BIOLOGICAL EVALUATION ; CANCER-CHEMOTHERAPY ; ANTICANCER AGENTS ; ANGIOGENESIS ; TARGETS ; DISCOVERY ; APOPTOSIS ; DNA ; COMBINATION |
| 资助项目 | National Basic Research Program of China (973 Program)[2010CB126100] ; National High Technology Research and Development Program of China (863 Program)[2011AA10A207] ; National Natural Science Foundation of China[81173080] ; Shanghai Committee of Science and Technology[10431902600] ; Shanghai Committee of Science and Technology[11DZ2260600] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000322850100046 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277551]  |
| 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 | Chen, Zhuo |
| 作者单位 | 1.E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai Key Lab Chem Biol, Shanghai Key Lab New Drug Design,Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Xin,Chen, Zhuo,Tong, Linjiang,et al. Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs)[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,65:477-486. |
| APA | Wang, Xin.,Chen, Zhuo.,Tong, Linjiang.,Tan, Shaoying.,Zhou, Wei.,...&Xu, Yufang.(2013).Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs).EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,65,477-486. |
| MLA | Wang, Xin,et al."Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs)".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 65(2013):477-486. |
入库方式： OAI收割
来源：上海药物研究所
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