具有不同长度 4-羟烷基胺侧链的萘酰亚胺的 DNA 结合和抗癌活性。
DNA binding and anticancer activity of naphthalimides with 4-hydroxyl-alkylamine side chains at different lengths.
机构信息
Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China; Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):937-41. doi: 10.1016/j.bmcl.2011.12.018. Epub 2011 Dec 8.
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 IC(50) values of 5.57 and 9.17μM, 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.
一系列新型萘酰亚胺衍生物在 4-位被各种羟烷基胺修饰。通过紫外可见光谱、荧光光谱和圆二色（CD）光谱及热变性研究了它们与 DNA 的结合性质。结果表明，化合物 3a-e 作为 DNA 嵌入剂与 Ct-DNA 具有中等结合亲和力。初步评价了 3a-e 的抗癌活性，化合物 3c 和 3e 对 Bel-7402 细胞系表现出较强的抗癌活性，IC50 值分别为 5.57 和 9.17μM。更有趣的是，在 3a-e 与 Ct-DNA 的复合物中发现了荧光发射的增强，特别是 3c。这将使这些化合物成为潜在的 DNA 染色剂。
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