Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation
Tan, Shaoying1; Han, Kun2; Li, Qiang1; Tong, Linjiang2; Yang, Yiqi1; Chen, Zhuo1; Xie, Hua2; Ding, Jian2; Qian, Xuhong1; Xu, Yufang1
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2014-10-06
卷号85页码:207-214
关键词Metal complexes Naphthalimide Cyclam RTK inhibitors Antiproliferation Antiangiogenesis
ISSN号0223-5234
DOI10.1016/j.ejmech.2014.07.068
文献子类Article
英文摘要A novel series of metal complexes of naphthalimide-cyclam conjugates were synthesized and their in vitro antitumor activities were evaluated. The newly-synthesized compounds showed huge diversity of antiproliferative potency due to variety of metal ions and length of alkyl chains, among which the Zn(II) and Cr(III) complexes exhibited comparable antiproliferative activities with amonafide via multiple tyrosine kinase inhibition. Further research revealed that the representative compound 8a displayed broad-spectrum antiproliferative activity against 15 cancer cell lines with average IC50 value 10.18 +/- 3.25 mu M, and effective antiangiogenic activity on human microvascular endothelial cells (HMEC-1). In brief, metal complexes of naphthalimide-cyclam conjugates were firstly designed and synthesized as multi-target tyrosine kinase inhibitors and proved of their antitumor capacities. (C) 2014 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[21236002] ; National Natural Science Foundation of China[21302054] ; National Science & Technology Pillar Program[00000000] ; Shanghai Committee of Science and Technology[13ZR1453100] ; Fundamental Research Funds for the Central Universities[00000000]
WOS关键词RENAL-CELL CARCINOMA ; CANCER-THERAPY ; GROWTH-FACTOR ; TOPOISOMERASE-II ; ANTITUMOR AGENTS ; IN-VITRO ; DERIVATIVES ; ANGIOGENESIS ; STRATEGIES ; SU11248
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:000342859700017
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/276872]  
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, Shanghai Key Lab New Drug Design, Shanghai Key Lab Chem Biol, State Key Lab Bioreactor Engn,Sch Pharm, Shanghai 200237, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China
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Tan, Shaoying,Han, Kun,Li, Qiang,et al. Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,85:207-214.
APA Tan, Shaoying.,Han, Kun.,Li, Qiang.,Tong, Linjiang.,Yang, Yiqi.,...&Xu, Yufang.(2014).Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,85,207-214.
MLA Tan, Shaoying,et al."Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 85(2014):207-214.
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