Autor según el artículo: Castro, Jessica; Bravo, Marlon; Alberti, Meritxell; Marsal, Anais; Jose Alonso-De Gennaro, Maria; Martinez-Ferrate, Oriol; Claver, Carmen; van Leeuwen, Piet W N M; Romero, Isabel; Benito, Antoni; Vilanova, Maria
Departamento: Química Física i Inorgànica
Autor/es de la URV: Claver Cabrero, Maria del Carmen Orosia
Palabras clave: Anticancer Apoptosis Cytotoxic mechanism Dinuclear iron (ii) compounds Iminopyridine ligands Inhibition of cell migration Selectivity for tumor cells
Resumen: A family of dinuclear iron (II) compounds with iminopyridine-based ligands displays selective cytotoxic activity against cancer cell lines. All compounds have IC50 values 2-6 fold lower than that of cisplatin, and 30-90 fold lower than that of carboplatin for the tumor cell lines assayed. Comparing the IC50 values between tumor and non-tumor cell lines, the selectivity indexes range from 3.2 to 34, compound 10, [Fe-2(4)(2)(CH3CN)(4)](BF4)(4), showing the highest selectivity. Those compounds carrying substituents on the iminopyridine ring show the same cytotoxicity as those without substituents. However, the electronic effects of the substituents on position 6 may be important for the cytotoxicity of the complexes, and consequently for their selectivity. All compounds act over DNA, promoting cuts on both strands in the presence of reactive oxygen species. Since compound 10 presented the highest selectivity, its cytotoxic effect was further characterized. It induces apoptosis, affects cell cycle phase distribution in a cell-dependent manner, and its cytotoxic effect is linked to reactive oxygen species generation. In addition, it decreases tumor cell migration, showing potential antimetastatic effects. These properties make compound 10 a good lead antitumor agent among all compounds studied here.
Áreas temáticas: Biotecnología Ciências biológicas i Ciências biológicas ii Ciências biológicas iii Farmacia Medicina ii Pharmaceutical science Pharmacology & pharmacy
Acceso a la licencia de uso: https://creativecommons.org/licenses/by/3.0/es/
Direcció de correo del autor: carmen.claver@urv.cat
Identificador del autor: 0000-0002-2518-7401
Fecha de alta del registro: 2024-10-12
Versión del articulo depositado: info:eu-repo/semantics/publishedVersion
Enlace a la fuente original: https://www.mdpi.com/1999-4923/14/12/2801
Referencia al articulo segun fuente origial: Pharmaceutics. 14 (12): 2801-
Referencia de l'ítem segons les normes APA: Castro, Jessica; Bravo, Marlon; Alberti, Meritxell; Marsal, Anais; Jose Alonso-De Gennaro, Maria; Martinez-Ferrate, Oriol; Claver, Carmen; van Leeuwen (2022). Dinuclear Iron Complexes of Iminopyridine-Based Ligands as Selective Cytotoxins for Tumor Cells and Inhibitors of Cancer Cell Migration. Pharmaceutics, 14(12), 2801-. DOI: 10.3390/pharmaceutics14122801
URL Documento de licencia: https://repositori.urv.cat/ca/proteccio-de-dades/
DOI del artículo: 10.3390/pharmaceutics14122801
Entidad: Universitat Rovira i Virgili
Año de publicación de la revista: 2022
Tipo de publicación: Journal Publications