DNA binding and anticancer activity of naphthalimides with 4-hydroxyl-alkylamine side chains at different lengths

被引:37
|
作者
Wang, Kerang [1 ,2 ]
Wang, Yueqing [1 ]
Yan, Xinhao [1 ]
Chen, Hua [1 ]
Ma, Gang [1 ]
Zhang, Pingzhu [1 ]
Li, Jinmei [2 ,3 ]
Li, Xiaoliu [1 ,2 ]
Zhang, Jinchao [1 ]
机构
[1] Hebei Univ, Key Lab Chem Biol Hebei Prov, Coll Chem & Environm Sci, Baoding 071002, Peoples R China
[2] Hebei Univ, Key Lab Med Chem & Mol Diag, Minist Educ, Baoding 071002, Peoples R China
[3] First Cent Hosp Baoding, Dept Pathol, Baoding 071000, Peoples R China
基金
中国国家自然科学基金;
关键词
Naphthalimide; DNA binding; Fluorescence; Anticancer; Hydroxyl-alkylamine; DESIGN; INTERCALATORS; DERIVATIVES; UNBS5162; ANALOGS; AGENTS;
D O I
10.1016/j.bmcl.2011.12.018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel naphthalimide derivatives modified with various hydroxyl-alkylamines at 4-position have been synthesized. Their DNA binding properties were investigated by UV-Vis, fluoescence, and circular dichroism (CD) spectroscopies and thermal denaturation. The results showed that compounds 3a-e as the DNA intercalator exhibited middle binding affinities with Ct-DNA. The anticancer activities of 3a-e were preliminarily evaluated, compounds 3c and 3e exhibited potent anticancer activities against Bel-7402 cell line with IC50 values of 5.57 and 9.17 mu M, respectively. More interestingly, enhancement of the fluorescence emission was found in the complexes of 3a-e with Ct-DNA, especially for 3c. This would make these compounds as potential DNA staining agents. (C) 2011 Elsevier Ltd. All rights reserved.
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页码:937 / 941
页数:5
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