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

Alshimaa I ZakiAdrienn SiposIstván KacsirNóra Ildikó KovácsÉva KerekesEvelin SzotákCsongor FreytagMáté DeményIstván RévészPéter BuglyóAttila BényeiEszter Anna JankaGábor KardosLászló SomsákPeter Bai^*Éva Bokor

• University of Debrecen, Debrecen, Hungary

Although, platinum-based complexes play aare pivotal role in chemotherapy regimens, their applicability 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 (MRSA and 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.Platinum-based remediesagents, as cisplatin, oxaliplatin, carboplatin, represent pillars of chemotherapy regimens against numerous solid tumors and hematological malignancies (Kenny and