2026-04-28T23:54:33Zhttps://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
Rubio Antolin, Ana Rosa
491
600
0000-0002-8504-9692
González, Rocío
4f1604f6-e341-4048-9097-7d799802f0d3
Busto Vázquez, Natalia
83
600
0000-0001-9637-1209
Vaquero Gutiérrez, Mónica
569
600
0000-0002-4550-4072
Iglesias, Ana L.
fc086dda-42c5-42b0-a694-6a0d07667547
Jalón Sotés, Félix Ángel
83a58ec8-3904-4c18-838c-bcdaf7357757
600
Espino Ordóñez, Gustavo
162
600
0000-0001-5617-5705
Rodríguez, Ana M.
64013be0-a1f8-4eba-8154-e6f7c49a9c55
García Ruiz, Begoña
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600
0000-0002-0817-1651
Manzano, Blanca R. .
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600
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
Spanish Ministerio de Ciencia, Innovación y UniversidadesFEDER (RTI2018-100709-B-C21 and RTI2018-102040-B-100), Junta de Comunidades de CastillaLa Mancha-FEDER (JCCM) (grant SBPLY/19/180501/000260), Junta de Castilla y León-FEDER (BU087G19 and BU305P18), “la Caixa” Foundation (LCF/PR/PR12/11070003), as well as by UCLMFEDER (grants 2019-GRIN-27183 and 2019-GRIN-27209).
application/pdf
eng
MDPI
Pharmaceutics. 2021, V. 13, n. 10, 1540
https://doi.org/10.3390/pharmaceutics13101540
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-100709-B-C21/ES/NUEVOS METALOFARMACOS DISEÑADOS PARA INCREMENTAR LA SELECTIVIDAD EN TRATAMIENTOS CONTRA EL CANCER. USO DE FOTOTERAPIA Y VEHICULIZACION CON LIGANDOS DIRIGIDOS A TUMORES
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-102040-B-I00/ES/PROPIEDADES ANTIMICROBIANAS DE NUEVOS COMPLEJOS ORGANOMETALICOS
info:eu-repo/grantAgreement/JCCM//SBPLY%2F19%2F180501%2F000260
info:eu-repo/grantAgreement/Junta de Castilla y León//BU087G19
info:eu-repo/grantAgreement/Junta de Castilla y León//BU305P18
info:eu-repo/grantAgreement/Fundación Bancaria Caixa d'Estalvis i Pensions de Barcelona//LCF%2FPR%2FPR12%2F11070003
info:eu-repo/grantAgreement/UCLM//2019-GRIN-27183
info:eu-repo/grantAgreement/UCLM//2019-GRIN-27209
Atribución 4.0 Internacional
http://creativecommons.org/licenses/by/4.0/
info:eu-repo/semantics/openAccess
Chrysin ligands
Iridium
Ruthenium
Rhodium
Cancer
Metallodrugs
Piperidine
Half-sandwich
Bioquímica
Química inorgánica
Química física
Biochemistry
Chemistry, Inorganic
Chemistry, Physical and theoretical
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
info:eu-repo/semantics/publishedVersion
Pharmaceutics
13
10
1540
THUMBNAIL
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LICENSE
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ORIGINAL
Rubio-pharmaceutics_2021.pdf
Rubio-pharmaceutics_2021.pdf
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10259/6825
oai:riubu.ubu.es:10259/6825
2026-02-06 13:50:50.446
Repositorio Institucional de la Universidad de Burgos
bubrep@ubu.es
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