3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3
Forskningsoutput: Tidskriftsbidrag › Artikel i vetenskaplig tidskrift
Abstract
Copper(I)-catalyzed addition of alkynes to methyl 3-azido-3-deoxy-1-thio-β-d-galactopyranoside afforded stable and structurally simple 3-deoxy-3-(1H-1,2,3-triazol-1-yl)-1-thio-galactosides carrying a panel of substituents at the triazole C4 in high yields. The 3-(1H-[1,2,3]-triazol-1-yl)-1-thio-galactoside collection synthesized contained inhibitors of the tumor- and inflammation-related galectin-3 with Kd values as low as 107 μM, which is as potent as the natural disaccharide inhibitors lactose and N-acetyllactosamine.
Detaljer
Författare | |
---|---|
Enheter & grupper | |
Forskningsområden | Ämnesklassifikation (UKÄ) – OBLIGATORISK
|
Originalspråk | engelska |
---|---|
Sidor (från-till) | 3344-3346 |
Tidskrift | Bioorganic & Medicinal Chemistry Letters |
Volym | 15 |
Utgåva nummer | 14 |
Status | Published - 2005 |
Publikationskategori | Forskning |
Peer review utförd | Ja |