2026-05-30T14:24:00Zhttps://riubu.ubu.es/oai/requestoai:riubu.ubu.es:10259/68252026-02-06T12:50:50Zcom_10259_4363com_10259_5086com_10259_2604com_10259_4365col_10259_4364col_10259_4366
Repositorio Institucional de la Universidad de Burgos
author
Rubio Antolin, Ana Rosa
author
González, Rocío
author
Busto Vázquez, Natalia
author
Vaquero Gutiérrez, Mónica
author
Iglesias, Ana L.
author
Jalón Sotés, Félix Ángel
author
Espino Ordóñez, Gustavo
author
Rodríguez, Ana M.
author
García Ruiz, Begoña
author
Manzano, Blanca R. .
2022-09-01T08:24:11Z
2022-09-01T08:24:11Z
2021-09
1999-4923
http://hdl.handle.net/10259/6825
10.3390/pharmaceutics13101540
1999-4923
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
eng
Atribución 4.0 Internacional
Chrysin ligands
Iridium
Ruthenium
Rhodium
Cancer
Metallodrugs
Piperidine
Half-sandwich
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
info:eu-repo/semantics/article
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URL
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