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    Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10259/6825

    Título
    Anticancer Activity of Half-Sandwich Ru, Rh and Ir Complexes with Chrysin Derived Ligands: Strong Effect of the Side Chain in the Ligand and Influence of the Metal
    Autor
    Rubio Antolin, Ana RosaUBU authority Orcid
    González, Rocío
    Busto Vázquez, NataliaUBU authority Orcid
    Vaquero Gutiérrez, MónicaUBU authority Orcid
    Iglesias, Ana L.
    Jalón, Félix A.
    Espino Ordóñez, GustavoUBU authority Orcid
    Rodríguez, Ana M.
    García Ruiz, BegoñaUBU authority Orcid
    Manzano, Blanca R. .
    Publicado en
    Pharmaceutics. 2021, V. 13, n. 10, 1540
    Editorial
    MDPI
    Fecha de publicación
    2021-09
    ISSN
    1999-4923
    DOI
    10.3390/pharmaceutics13101540
    Abstract
    An important challenge in the field of anticancer chemotherapy is the search for new species to overcome the resistance of standard drugs. An interesting approach is to link bioactive ligands to metal fragments. In this work, we have synthesized a set of p-cymene-Ru or cyclopentadienyl-M (M = Rh, Ir) complexes with four chrysin-derived pro-ligands with different -OR substituents at position 7 of ring A. The introduction of a piperidine ring on chrysin led to the highly cytotoxic pro-ligand HL4 and its metal complexes L4-M (SW480 and A549 cell lines, cytotoxic order: L4-Ir > L4-Ru ≈ L4-Rh). HL4 and its complexes induce apoptosis and can overcome cis-platinum resistance. However, HL4 turns out to be more cytotoxic in healthy than in tumor cells in contrast to its metal complexes which displayed higher selectivity than cisplatin towards cancer cells. All L4-M complexes interact with double stranded DNA. Nonetheless, the influence of the metal is clear because only complex L4-Ir causes DNA cleavage, through the generation of highly reactive oxygen species (1O2 ). This result supports the hypothesis of a potential dual mechanism consisting of two different chemical pathways: DNA binding and ROS generation. This behavior provides this complex with a great effectivity in terms of cytotoxicity
    Palabras clave
    Chrysin ligands
    Iridium
    Ruthenium
    Rhodium
    Cancer
    Metallodrugs
    Piperidine
    Half-sandwich
    Materia
    Bioquímica
    Biochemistry
    Química inorgánica
    Chemistry, Inorganic
    Química física
    Chemistry, Physical and theoretical
    URI
    http://hdl.handle.net/10259/6825
    Versión del editor
    https://doi.org/10.3390/pharmaceutics13101540
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    Atribución 4.0 Internacional
    Documento(s) sujeto(s) a una licencia Creative Commons Atribución 4.0 Internacional
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    Nombre:
    Rubio-pharmaceutics_2021.pdf
    Tamaño:
    6.418Mb
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