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Molecules 2018, 23(8), 2017; https://doi.org/10.3390/molecules23082017

Synthesis and Preliminary Evaluation of Biological Activity of Glycoconjugates Analogues of Acyclic Uridine Derivatives

1
Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Faculty of Chemistry, Silesian University of Technology, Krzywoustego 4, 44-100 Gliwice, Poland
2
Biotechnology Center, Silesian University of Technology, Krzywoustego 8, 44-100 Gliwice, Poland
3
Department of Recombinant Vaccines, Intercollegiate Faculty of Biotechnology, University of Gdansk and Medical University of Gdansk, Abrahama 58, 80-307 Gdansk, Poland
*
Authors to whom correspondence should be addressed.
Received: 23 July 2018 / Revised: 9 August 2018 / Accepted: 11 August 2018 / Published: 13 August 2018
(This article belongs to the Collection Advances in Carbohydrate Chemistry)
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Abstract

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. View Full-Text
Keywords: glycosyltransferases; glycosyltransferase inhibitors; glycoconjugates; acyclic uridine derivatives; thioglycosides glycosyltransferases; glycosyltransferase inhibitors; glycoconjugates; acyclic uridine derivatives; thioglycosides
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Komor, R.; Pastuch-Gawolek, G.; Krol, E.; Szeja, W. Synthesis and Preliminary Evaluation of Biological Activity of Glycoconjugates Analogues of Acyclic Uridine Derivatives. Molecules 2018, 23, 2017.

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