Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs)

doi:10.1016/j.ejmech.2013.05.002

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	Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs)
	Wang, Xin1 ; Chen, Zhuo 1,2; Tong, Linjiang 2; Tan, Shaoying 1; Zhou, Wei 1; Peng, Ting 2; Han, Kun 2; Ding, Jian2 ; Xie, Hua2 ; Xu, Yufang 1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	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.
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关键词	ANTITUMOR AGENTS ; BIOLOGICAL EVALUATION ; CANCER-CHEMOTHERAPY ; ANTICANCER AGENTS ; ANGIOGENESIS ; TARGETS ; DISCOVERY ; APOPTOSIS ; DNA ; COMBINATION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000322850100046
内容类型	期刊论文
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.