Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: synthesis and biological evaluation.
Novel metal complexes of naphthalimide-cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: synthesis and biological evaluation.
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DOI：
10.1016/j.ejmech.2014.07.068
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发表时间：
2014-10
影响因子：
6.7
通讯作者：
Shaoying Tan;Kun Han;Qiang Li;Lin-jiang Tong;Yiqi Yang;Zhuo Chen;Hua Xie;Jian Ding;X. Qian;Yufang Xu
中科院分区：
文献类型：
--
作者：
Shaoying Tan;Kun Han;Qiang Li;Lin-jiang Tong;Yiqi Yang;Zhuo Chen;Hua Xie;Jian Ding;X. Qian;Yufang Xu
A novel series of metal complexes of naphthalimide–cyclam conjugates were synthesized and theirin vitroantitumor 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 compound8adisplayed broad-spectrum antiproliferative activity against 15 cancer cell lines with average IC50value 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.
