Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines

In this study we report the synthesis, characterization and a thorough biological evaluation of twelve organoruthenium–8-hydroxyquinolinato (Ru-hq) complexes. The chosen hqH ligands bear various halogen atoms in different positions which enables to study effect of the substituents on physico-chemica...

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Detalles Bibliográficos
Autores principales: Kljun, Jakob, León, Ignacio Esteban, Pervi, Spela, Cadavid Vargas, Juan Fernando, Etcheverry, Susana Beatriz, He, Weijiang, Bai, Yang, Turel, Iztok
Formato: Articulo Preprint
Lenguaje:Inglés
Publicado: 2018
Materias:
Bioquímica
Quinolines
Ruthenium
Cancer
Complexes
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/97087
https://ri.conicet.gov.ar/11336/87546
Aporte de:
SEDICI (UNLP) de Universidad Nacional de La Plata
id I19-R120-10915-97087
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Bioquímica
Quinolines
Ruthenium
Cancer
Complexes
spellingShingle Bioquímica
Quinolines
Ruthenium
Cancer
Complexes
Kljun, Jakob
León, Ignacio Esteban
Pervi, Spela
Cadavid Vargas, Juan Fernando
Etcheverry, Susana Beatriz
He, Weijiang
Bai, Yang
Turel, Iztok
Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
topic_facet Bioquímica
Quinolines
Ruthenium
Cancer
Complexes
description In this study we report the synthesis, characterization and a thorough biological evaluation of twelve organoruthenium–8-hydroxyquinolinato (Ru-hq) complexes. The chosen hqH ligands bear various halogen atoms in different positions which enables to study effect of the substituents on physico-chemical and biological properties. The determined crystal structures of novel complexes expectedly show the cymene ring, a bidentately coordinated deprotonated hq and a halide ligand (chlorido or iodido) coordinated to the ruthenium central ion. In previous studies the anticancer potential of organoruthenium complex with 8-hydroxyquinoline ligand clioquinol was well established and we have decided to perform an extended biological evaluation (antibacterial and antitumor activity) of the whole series of halo-substituted analogs. Beside the cytotoxic potential of studied compounds also the effect of two selected complexes (9 and 10) on apoptosis induction in MG-63 and A549 cells was also studied via externalization of phosphatidylserine at the outer plasma membrane leaflet. Both selected complexes that gave best preliminary cytotoxicity results contain bromo substituted hq ligands. Apoptosis induction results are in agreement with the cell viability assays suggesting the higher and more selective anticancer activity of complex 10 in comparison to complex 9 on MG-63 cells.
format Articulo
Preprint
author Kljun, Jakob
León, Ignacio Esteban
Pervi, Spela
Cadavid Vargas, Juan Fernando
Etcheverry, Susana Beatriz
He, Weijiang
Bai, Yang
Turel, Iztok
author_facet Kljun, Jakob
León, Ignacio Esteban
Pervi, Spela
Cadavid Vargas, Juan Fernando
Etcheverry, Susana Beatriz
He, Weijiang
Bai, Yang
Turel, Iztok
author_sort Kljun, Jakob
title Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
title_short Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
title_full Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
title_fullStr Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
title_full_unstemmed Synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
title_sort synthesis and biological characterization of organoruthenium complexes with 8-hydroxyquinolines
publishDate 2018
url http://sedici.unlp.edu.ar/handle/10915/97087
https://ri.conicet.gov.ar/11336/87546
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bdutipo_str Repositorios
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