Journal
MOLECULES
Volume 24, Issue 19, Pages -Publisher
MDPI
DOI: 10.3390/molecules24193520
Keywords
LDH inhibitors; glycoconjugates; anticancer agents
Funding
- MIUR-Italy (PRIN 2015) [2015RNWJAM_003]
- University of Pisa [PRA_2018_18]
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Conjugation of known biologically active molecules to carbohydrate frameworks represents a valuable option for the preparation of hybrid, structurally-related families of compounds with the aim of modulating their biological response. Therefore, we present here a study on the preparation of d-galacto, d-manno, d-gluco, and d-lactose glycoconjugates of an established N-hydroxyindole-based (NHI) inhibitor of lactated dehydrogenase (LDH). Structural variations involved the sugar stereochemistry and size as well as the anchoring point of the NHI on the carbohydrate frame (either C-1 or C-6). In the case of the galactose anomeric glycoconjugate (C-1), intriguing solvent-dependent effects were observed in the glycosylation stereochemical outcome. The biological activity of the deprotected glycoconjugates in contrasting lactate formation and cancer cell proliferation are described.
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