RT info:eu-repo/semantics/article
T1 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
A1 Rubio Antolin, Ana Rosa
A1 González, Rocío
A1 Busto Vázquez, Natalia
A1 Vaquero Gutiérrez, Mónica
A1 Iglesias, Ana L.
A1 Jalón, Félix A.
A1 Espino Ordóñez, Gustavo
A1 Rodríguez, Ana M.
A1 García Ruiz, Begoña
A1 Manzano, Blanca R. .
K1 Chrysin ligands
K1 Iridium
K1 Ruthenium
K1 Rhodium
K1 Cancer
K1 Metallodrugs
K1 Piperidine
K1 Half-sandwich
K1 Bioquímica
K1 Biochemistry
K1 Química inorgánica
K1 Chemistry, Inorganic
K1 Química física
K1 Chemistry, Physical and theoretical
AB An important challenge in the field of anticancer chemotherapy is the search for new speciesto overcome the resistance of standard drugs. An interesting approach is to link bioactive ligands tometal 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 atposition 7 of ring A. The introduction of a piperidine ring on chrysin led to the highly cytotoxicpro-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 metalcomplexes which displayed higher selectivity than cisplatin towards cancer cells. All L4-M complexesinteract with double stranded DNA. Nonetheless, the influence of the metal is clear because onlycomplex 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 chemicalpathways: DNA binding and ROS generation. This behavior provides this complex with a greateffectivity in terms of cytotoxicity
PB MDPI
SN 1999-4923
YR 2021
FD 2021-09
LK http://hdl.handle.net/10259/6825
UL http://hdl.handle.net/10259/6825
LA eng
NO 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).
DS Repositorio Institucional de la Universidad de Burgos
RD 24-abr-2024