8-Hydroxyquinoline scaffold is a privileged structure used in designing a new active agents with therapeutic potential. Its connections with the sugar unit is formed to improve the pharmacokinetic properties. The broad spectrum of activity of quinoline derivatives, especially glycoconjugates, is often associated with the ability to chelate metal ions or with the ability to intercalate into DNA. Simple and effective methods of synthesis glycoconjugates of 8-hydroxyquinoline and 8-hydroxyquinaldine derivatives, containing an O-glycosidic bond or a 1,2,3-triazole linker in their structure, have been developed. The obtained glycoconjugates were tested for their ability to inhibit β-1,4-Galactosyltransferase, as well as inhibit cancer cell proliferation. It was found that used glycoconjugation strategy influenced both improvement of activity and improvement of the bioavailability of 8-HQ derivatives. Their activity depends on type of attached sugar, presence of protecting groups in sugar moiety and presence of a linker between sugar and quinolone aglycone.

中文翻译：

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8-羟基喹啉糖缀合物的合成及其β1,4-GalT抑制和抗癌特性的初步测定。

8-羟基喹啉支架是一种特权结构，用于设计具有治疗潜力的新型活性剂。其与糖单元的连接被形成以改善药代动力学性质。喹啉衍生物，尤其是糖缀合物的广谱活性通常与螯合金属离子的能力或与插入DNA的能力有关。已经开发了简单有效的合成8-羟基喹啉和8-羟基喹哪啶衍生物的糖缀合物的方法，所述糖缀合物在其结构中包含O-糖苷键或1,2,3-三唑接头。测试获得的糖缀合物抑制β-1，4-半乳糖基转移酶以及抑制癌细胞增殖的能力。发现使用的糖缀合策略既影响活性的提高又影响8-HQ衍生物的生物利用度的提高。它们的活性取决于附着的糖的类型，糖部分中保护基的存在以及糖和喹诺酮苷元之间的连接基的存在。