Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3
A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the
discovery of highly selective and high affinity (Kd down to 11 μM) small monosaccharide …
discovery of highly selective and high affinity (Kd down to 11 μM) small monosaccharide …
Synthesis of O-galactosyl aldoximes as potent LacNAc-mimetic galectin-3 inhibitors
J Tejler, H Leffler, UJ Nilsson - Bioorganic & medicinal chemistry letters, 2005 - Elsevier
A panel of anomeric oxime ether derivatives of β-galactose were synthesized via the
reaction of O-β-d-galactopyranosylhydroxylamine with aldehydes. The oxime ethers were …
reaction of O-β-d-galactopyranosylhydroxylamine with aldehydes. The oxime ethers were …
1H-1, 2, 3-triazol-1-yl thiodigalactoside derivatives as high affinity galectin-3 inhibitors
BA Salameh, I Cumpstey, A Sundin, H Leffler… - Bioorganic & medicinal …, 2010 - Elsevier
Galactose C3-triazole derivatives were synthesized by Cu (I)-catalyzed cycloaddition
between acetylenes and galactose C3-azido derivatives. Evaluation against galectin-3, 7 …
between acetylenes and galactose C3-azido derivatives. Evaluation against galectin-3, 7 …
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of …
C Liu, W Wang, J Feng, B Beno, T Raja… - Bioorganic & Medicinal …, 2024 - Elsevier
As a result of our continued efforts to pursue Gal-3 inhibitors that could be used to fully
evaluate the potential of Gal-3 as a therapeutic target, two novel series of benzothiazole …
evaluate the potential of Gal-3 as a therapeutic target, two novel series of benzothiazole …
Discovery of selective and orally available galectin-1 inhibitors
FR Zetterberg, C Diehl, M Håkansson… - Journal of Medicinal …, 2023 - ACS Publications
A new series of orally available α-d-galactopyranosides with high affinity and specificity
toward galectin-1 have been discovered. High affinity and specificity were achieved by …
toward galectin-1 have been discovered. High affinity and specificity were achieved by …
Synthesis of galactose-mimicking 1H-(1, 2, 3-triazol-1-yl)-mannosides as selective galectin-3 and 9N inhibitors
J Tejler, F Skogman, H Leffler, UJ Nilsson - Carbohydrate research, 2007 - Elsevier
1H-[1, 2, 3]-Triazol-1-yl mannosides have been synthesized as inhibitors for the β-
galactoside-binding family of galectin proteins. Easier synthetic access to C1 in mannose, as …
galactoside-binding family of galectin proteins. Easier synthetic access to C1 in mannose, as …
Design and synthesis of novel 3-triazolyl-1-thiogalactosides as galectin-1,-3 and-8 inhibitors
Galectins are galactoside-binding proteins that play a role in various pathophysiological
conditions, making them attractive targets in drug discovery. We have designed and …
conditions, making them attractive targets in drug discovery. We have designed and …
[HTML][HTML] Synthetic 1, 2, 3-triazole-linked glycoconjugates bind with high affinity to human galectin-3
This work describes the synthesis of the 1, 2, 3-triazole amino acid-derived-3-O-galactosides
1–6 and the 1, 2, 3-triazole di-lactose-derived glycoconjugate 7 as potential galectin-3 …
1–6 and the 1, 2, 3-triazole di-lactose-derived glycoconjugate 7 as potential galectin-3 …
Low Micromolar Inhibitors of Galectin‐3 Based on 3′‐Derivatization of N‐Acetyllactosamine
P Sörme, Y Qian, PG Nyholm, H Leffler… - …, 2002 - Wiley Online Library
A strategy for generating potential galectin inhibitors was devised based on derivatization at
the C‐3′ atom in 3′‐amino‐N‐acetyllactosamine by using structural knowledge of the …
the C‐3′ atom in 3′‐amino‐N‐acetyllactosamine by using structural knowledge of the …
Tuning the preference of thiodigalactoside-and lactosamine-based ligands to galectin-3 over galectin-1
H van Hattum, HM Branderhorst, EE Moret… - Journal of Medicinal …, 2013 - ACS Publications
Inhibitors for galectin-1 and-3 were synthesized from thiodigalactoside and lactosamine by
derivatization of the galactose C3. Introduction of 4-phenyl-1 H-1, 2, 3-triazol-1-yl …
derivatization of the galactose C3. Introduction of 4-phenyl-1 H-1, 2, 3-triazol-1-yl …