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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 02期

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