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N-heterocyclic-carbene vs diphosphine auxiliary ligands in thioamidato Cu(I) and Ag(I) complexes towards the development of potent and dual-activity antibacterial and apoptosis-inducing anticancer agents.
Varna, Despoina; Geromichalos, George; Gioftsidou, Dimitra K; Tzimopoulos, Demetrios; Hatzidimitriou, Antonios G; Dalezis, Panagiotis; Papi, Rigini; Trafalis, Dimitrios; Angaridis, Panagiotis A.
Afiliación
  • Varna D; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
  • Geromichalos G; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
  • Gioftsidou DK; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
  • Tzimopoulos D; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
  • Hatzidimitriou AG; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
  • Dalezis P; Laboratory of Pharmacology, Medical School, National and Kapodistrian University of Athens, 75 Mikras Asias Street, 11527 Athens, Greece.
  • Papi R; Laboratory of Biochemistry, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.
  • Trafalis D; Laboratory of Pharmacology, Medical School, National and Kapodistrian University of Athens, 75 Mikras Asias Street, 11527 Athens, Greece. Electronic address: dtrafal@med.uoa.gr.
  • Angaridis PA; Laboratory of Inorganic Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece. Electronic address: panosangaridis@chem.auth.gr.
J Inorg Biochem ; 252: 112472, 2024 03.
Article en En | MEDLINE | ID: mdl-38215535
ABSTRACT
Group 11 metal complexes exhibit promising antibacterial and anticancer properties which can be further enhanced by appropriate ligands. Herein, a series of mononuclear thioamidato Cu(I) and Ag(I) complexes bearing either a diphosphine (P^P) or a N-heterocyclic carbene (NHC) auxiliary ligand (L) was synthesized, and the impact of the co-ligand L on the in vitro antibacterial and anticancer properties of their complexes was assessed. All complexes effectively inhibited the growth of various bacterial strains, with the NHC-Cu(I) complex found to be particularly effective against the Gram (+) bacteria (IC50 = 1-4 µg mL-1). Cytotoxicity studies against various human cancer cells revealed their high anticancer potency and the superior activity of the NHC-Ag(I) complex (IC50 = 0.95-4.5 µΜ). Flow cytometric analysis on lung and breast cancer cells treated with the NHC-Ag(I) complex suggested an apoptotic cell-death pathway; molecular docking calculations provided mechanistic insights, proving the capacity of the complex to bind on apoptosis-regulating proteins and affect their functionalities.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Complejos de Coordinación / Compuestos Heterocíclicos / Antineoplásicos Límite: Humans Idioma: En Revista: J Inorg Biochem Año: 2024 Tipo del documento: Article País de afiliación: Grecia Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Complejos de Coordinación / Compuestos Heterocíclicos / Antineoplásicos Límite: Humans Idioma: En Revista: J Inorg Biochem Año: 2024 Tipo del documento: Article País de afiliación: Grecia Pais de publicación: Estados Unidos