Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Pharmacy, Ocean University of China, Qingdao 266003, China.
Int J Mol Sci. 2013 Aug 15;14(8):16851-65. doi: 10.3390/ijms140816851.
A series of novel potential DNA bis-intercalators were designed and synthesized, in which two glucuronic acids were linked by ethylenediamine, and the glucuronic acid was coupled with various chromophores, including quinoline, acridine, indole and purine, at the C-1 position. The preliminary binding properties of these compounds to calf thymus DNA (CT-DNA) have been investigated by UV-absorption and fluorescence spectroscopy. The results indicated that all the target compounds can interact with CT-DNA, and the acridine derivative, 3b, showed the highest key selection vector (KSV) value, which suggested that compound 3b binds most strongly to CT-DNA.
设计并合成了一系列新型潜在的 DNA 双嵌入剂，其中两个葡萄糖醛酸通过乙二胺连接，葡萄糖醛酸在 C-1 位与各种生色团偶联，包括喹啉、吖啶、吲哚和嘌呤。通过紫外吸收光谱和荧光光谱研究了这些化合物与小牛胸腺 DNA（CT-DNA）的初步结合性质。结果表明，所有目标化合物都可以与 CT-DNA 相互作用，吖啶衍生物 3b 显示出最高的关键选择向量（KSV）值，这表明化合物 3b 与 CT-DNA 结合最强。
