Platinum-group metal half-sandwich complexes of 1-(alpa-D-glucopyranosyl)-4-hetaryl-1,2,3-triazoles : synthesis, solution equilibrium studies and investigation of their anticancer and antimicrobial activitie

Salama, Alshimaa Ibrahim Zaki Ahmed and Sipos, Adrienn and Kacsir, István and Kovács, Nóra Ildikó and Kerekes, Éva and Szoták, Evelin and Freytag, Csongor and Demény, Máté Ágoston and Révész, István and Buglyó, Péter and Bényei, Attila Csaba and Janka, Eszter Anna and Kardos, Gábor and Somsák, László and Bay, Péter and Bokor, Éva (2025) Platinum-group metal half-sandwich complexes of 1-(alpa-D-glucopyranosyl)-4-hetaryl-1,2,3-triazoles : synthesis, solution equilibrium studies and investigation of their anticancer and antimicrobial activitie. FRONTIERS IN CHEMISTRY, 13. ISSN 2296-2646 (In Press)

Preview

Text fchem-13-1619991.pdf - Published Version Available under License Creative Commons Attribution. Download (5MB) | Preview

Abstract

Although platinum-based complexes are pivotal in chemotherapy, their clinical use is limited by toxicity and resistance. Previously, we identified a set of osmium, ruthenium, and iridium half-sandwich complexes of 1- N -(β- d -glucopyranosyl)-4-hetaryl-1,2,3-triazole-type N,N-chelators with potent and selective activity against a large set of diverse neoplasia cell models and multiresistant Gram-positive bacteria (methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE)). Our aim in this study was to assess how the configuration of the C1 carbon in the glucose moiety affects the biological activity of the complexes. Thus, 1- N -(α- d -glucopyranosyl)-4-hetaryl-1,2,3-triazoles were synthesized and used as N,N-bidentate ligands to result in half-sandwich type complexes analogous to the earlier reported ones. Overall, the newly prepared complexes with the α-anomeric carbohydrate moiety had similar biological properties to the complexes with the β-anomeric carbohydrate unit in terms of their biological activity on cancer cells or primary human cells. Importantly, the bacteriostatic property of the complexes with an α-anomeric sugar moiety was inferior to that of the complexes containing the β-anomer.

Actions (login required)

Edit Item