Next Article in Journal
Chemically Responsive Hydrogel Deformation Mechanics: A Review
Previous Article in Journal
Fermentation by Multiple Bacterial Strains Improves the Production of Bioactive Compounds and Antioxidant Activity of Goji Juice
Open AccessArticle

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

Dipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126 Pisa, Italy
Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via G. Moruzzi 3, 56124 Pisa, Italy
Authors to whom correspondence should be addressed.
Dedicated to the beloved memory of Prof. Cinzia Chiappe.
Molecules 2019, 24(19), 3520;
Received: 3 September 2019 / Revised: 26 September 2019 / Accepted: 27 September 2019 / Published: 28 September 2019
(This article belongs to the Section Bioorganic Chemistry)
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. View Full-Text
Keywords: LDH inhibitors; glycoconjugates; anticancer agents LDH inhibitors; glycoconjugates; anticancer agents
Show Figures

Graphical abstract

MDPI and ACS Style

D’Andrea, F.; Vagelli, G.; Granchi, C.; Guazzelli, L.; Tuccinardi, T.; Poli, G.; Iacopini, D.; Minutolo, F.; Di Bussolo, V. Synthesis and Biological Evaluation of New Glycoconjugated LDH Inhibitors as Anticancer Agents. Molecules 2019, 24, 3520.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

Search more from Scilit
Back to TopTop