Sjors van Klaveren (Author), Jaka Dernovšek (Author), Žiga Jakopin (Author), Marko Anderluh (Author), Hakon Leffler (Author), Ulf Nilsson (Author), Tihomir Tomašić (Author)

Abstract

Galectins are galactoside-binding proteins that play a role in various pathophysiological conditions, making them attractive targets in drug discovery. We have designed and synthesised a focused library of aromatic 3-triazolyl-1-thiogalactosides targeting their core site for binding of galactose and a subsite on its non-reducing side. Evaluation of their binding affinities for galectin-1, -3, and -8N identified acetamide-based compound 36 as a suitable compound for further affinity enhancement by adding groups at the reducing side of the galactose. Synthesis of its dichlorothiophenyl analogue 59 and the thiodigalactoside analogue 62 yielded promising pan-galectin inhibitors.

Keywords

β-galaktozid;galektini;raziskava zdravil;diklorotiofenilni analog 59;

Data

Language: English
Year of publishing:
Typology: 1.01 - Original Scientific Article
Organization: UL FFA - Faculty of Pharmacy
UDC: 615.4:54(057)
COBISS: 113857283 Link will open in a new window
ISSN: 2046-2069
Views: 1047
Downloads: 198
Average score: 0 (0 votes)
Metadata: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Other data

Secondary language: Slovenian
Secondary keywords: Zdravila;Farmacevtska kemija;
Type (COBISS): Article
Pages: str. 18973-18984
Volume: ǂVol. ǂ12
Issue: ǂiss. ǂ29
Chronology: 2022
DOI: 10.1039/D2RA03163A
ID: 16146520