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Synthesis and DNA-binding properties of novel DNA cyclo-intercalators containing purine-glucuronic acid hybrids

机译:含嘌呤-葡萄糖醛酸杂化物的新型DNA环嵌入剂的合成及DNA结合特性

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摘要

Novel DNA cyclo-intercalators, which incorporated two intercalator subunits linked by two bridges, were synthesized. Binding of the compounds to calf-thymus DNA was studied by fluorescence spectroscopy, and docking simulations were used to predict the binding modes of these cyclic compounds. The spectral data demonstrated that all of these compounds can interact with CT-DNA. The sugar moiety played an important role in the process of binding between the intercalators containing glucuronic acid and DNA. The length and flexibility of the connecting bridges affected the binding affinity of the resultant cyclo-intercalators. Docking simulations showed that compounds 7 and 8 interact with DNA as mono-intercalators. (C) 2016 Elsevier Ltd. All rights reserved.
机译:合成了新的DNA环嵌入剂,其中整合了由两个桥连接的两个嵌入剂亚基。通过荧光光谱研究了化合物与小牛胸腺DNA的结合,并使用对接模拟来预测这些环状化合物的结合模式。光谱数据表明所有这些化合物均可与CT-DNA相互作用。糖部分在含葡萄糖醛酸的嵌入剂与DNA之间的结合过程中起着重要作用。连接桥的长度和柔韧性影响所得环嵌入剂的结合亲和力。对接模拟表明,化合物7和8作为单嵌入剂与DNA相互作用。 (C)2016 Elsevier Ltd.保留所有权利。

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