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Synthesis and Biological Evaluation of New Glycoconjugated LDH Inhibitors as Anticancer Agents.

ABSTRACT: 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.

SUBMITTER: D'Andrea F 

PROVIDER: S-EPMC6804087 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature

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Synthesis and Biological Evaluation of New Glycoconjugated LDH Inhibitors as Anticancer Agents.

D'Andrea Felicia F   Vagelli Giulia G   Granchi Carlotta C   Guazzelli Lorenzo L   Tuccinardi Tiziano T   Poli Giulio G   Iacopini Dalila D   Minutolo Filippo F   Di Bussolo Valeria V  

Molecules (Basel, Switzerland) 20190928 19

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-<i>galacto</i>, d-<i>manno</i>, d-<i>gluco</i>, and d-<i>lactose</i> glycoconjugates of an established <i>N</i>-hydroxyindole-based (NHI) inhibitor of lactated dehydrogenase (LDH). Structural variations inv  ...[more]

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