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

Povzetek

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.

Ključne besede

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

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 615.4:54(057)
COBISS: 113857283 Povezava se bo odprla v novem oknu
ISSN: 2046-2069
Št. ogledov: 1047
Št. prenosov: 198
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Sekundarne ključne besede: Zdravila;Farmacevtska kemija;
Vrsta dela (COBISS): Članek v reviji
Strani: str. 18973-18984
Letnik: ǂVol. ǂ12
Zvezek: ǂiss. ǂ29
Čas izdaje: 2022
DOI: 10.1039/D2RA03163A
ID: 16146520