糖缀合物类似物的合成及初步生物活性评价非环尿嘧啶衍生物。

Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Faculty of Chemistry, Silesian University of Technology, Krzywoustego 4, 44-100 Gliwice, Poland.

Biotechnology Center, Silesian University of Technology, Krzywoustego 8, 44-100 Gliwice, Poland.

Molecules. 2018 Aug 13;23(8):2017. doi: 10.3390/molecules23082017.

Herein we present the methodology for obtaining glycosyltransferase inhibitors, analogues of natural enzyme substrates of donor-type: UDP-glucose and UDP-galactose. The synthesis concerned glycoconjugates, nucleoside analogues containing an acyclic ribose mimetic linked to a uracil moiety in their structure. The biological activity of the synthesised compounds was determined on the basis of their ability to inhibit the model enzyme action of β-1,4-galactosyltransferase from bovine milk. The obtained results allowed to expand and supplement the existing library of synthetic compounds that are able to regulate the biological activity of enzymes from the GT class.

在此，我们介绍了获得糖基转移酶抑制剂的方法，这些抑制剂是天然酶供体底物 UDP-葡萄糖和 UDP-半乳糖的类似物。该合成涉及糖缀合物，即核苷类似物，其结构中含有无环核糖类似物，与尿嘧啶部分相连。所合成化合物的生物活性是基于它们抑制牛乳腺中β-1,4-半乳糖基转移酶模型酶活性的能力来确定的。所获得的结果允许扩展和补充能够调节 GT 类酶生物活性的合成化合物的现有文库。