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Novel metal complexes of naphthalimide–cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation.

Authors :
Tan, Shaoying
Han, Kun
Li, Qiang
Tong, Linjiang
Yang, Yiqi
Chen, Zhuo
Xie, Hua
Ding, Jian
Qian, Xuhong
Xu, Yufang
Source :
European Journal of Medicinal Chemistry. Oct2014, Vol. 85, p207-214. 8p.
Publication Year :
2014

Abstract

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 IC 50 value 10.18 ± 3.25 μM, 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
85
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
98144936
Full Text :
https://doi.org/10.1016/j.ejmech.2014.07.068