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Design and synthesis of novel 3-triazolyl-1-thiogalactosides as galectin-1, -3 and -8 inhibitors [Elektronski vir]van Klaveren, Sjors ...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.Source: RSC advances [Elektronski vir]. - ISSN 2046-2069 (Vol. 12, iss. 29, 2022, str. 18973-18984)Type of material - e-article ; adult, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 113857283
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Author | van Klaveren, Sjors ... |
Title | Design and synthesis of novel 3-triazolyl-1-thiogalactosides as galectin-1, -3 and -8 inhibitors [Elektronski vir] |
Publication date | 2022-06-30 |
COBISS.SI-ID | 113857283 |
Publication version in repository | Unidentified |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Multidisciplinary European Joint Doctorate in the Design and Development of Glyco Drugs | PhD4GlycoDrug | 765581 |
European Commission |
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2022 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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van Klaveren, Sjors | ![]() |
Dernovšek, Jaka | 54784 |
Jakopin, Žiga | 26496 |
Anderluh, Marko | 21456 |
Leffler, Hakon | ![]() |
Nilsson, Ulf, farmacevt | ![]() |
Tomašič, Tihomir | 28334 |
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