Busca avançada
Ano de início
Entree


Impact of ligand esterification on the cytotoxicity against breast cancer cells of ruthenium(II)/dppb pyridinedicarboxylate complexes☆

Texto completo
Autor(es):
de Camargo, Mariana Santoro ; De Grandis, Rone Aparecido ; Galo, Ayrton Correa ; Resende, Flavia Aparecida ; Marcon, Pedro Henrique Salgado ; Ellena, Javier ; de Araujo-Netod, Joao Honorato ; Batista, Alzir Azevedo
Número total de Autores: 8
Tipo de documento: Artigo Científico
Fonte: Journal of Inorganic Biochemistry; v. 272, p. 10-pg., 2025-11-01.
Resumo

Here we report the synthesis and characterization of five new ruthenium(II) complexes with the general formula [Ru(N-O)2(dppb)], where dppb is 1,4-bis(diphenylphosphino)butane and the N-O ligands are derivatives of pyridinecarboxylic acids: picolinic acid (C20), 2,3- (C23), 2,4- (C24), and 2,5-pyridinedicarboxylic acids (C25), as well as the monoester derivative of 2,4-pyridinedicarboxylic acid (C24e), obtained by Fischer esterification. The complexes were characterized by elemental analysis, molar conductivity, cyclic voltammetry, NMR spectroscopy (1H and 31P{1H}), and single-crystal X-ray diffraction (for C23 and C24). The stability of the complexes in solution was confirmed by UV-Vis spectroscopy in DMSO and by 31P{1H} NMR in a DMSO/DMEM mixture (for C24), with no evidence of significant speciation reactions. Biological assays revealed that complexes C20 and C24e exhibit significant cytotoxic activity and selectivity against human breast cancer cell lines (MCF-7 and MDA-MB-231) over non-tumorigenic HaCaT cells. Notably, C20 remained active in three-dimensional spheroid models of MCF-7 cells, showing greater potency than cisplatin. Additionally, both C20 and C24e did not induce mutagenic effects or generate intracellular reactive oxygen species, suggesting alternative mechanisms of cytotoxicity. These findings support the potential of picolinic and esterified pyridinedicarboxylic acid ruthenium(II) complexes as promising antitumor agents. (AU)

Processo FAPESP: 17/16278-9 - Estudo do potencial genotoxicológico e da permeabilidade em células Caco-2 de complexos metálicos com promissoras atividades biológicas
Beneficiário:Flávia Aparecida Resende Nogueira
Modalidade de apoio: Auxílio à Pesquisa - Regular
Processo FAPESP: 21/04876-4 - Estudos sobre estrutura & atividade de complexos de RuII/areno/mercaptoligantes frente ao câncer
Beneficiário:João Honorato de Araujo Neto
Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
Processo FAPESP: 17/15850-0 - Difração de raios X como ferramenta no desenvolvimento de potenciais fármacos
Beneficiário:Eduardo Ernesto Castellano
Modalidade de apoio: Auxílio à Pesquisa - Temático
Processo FAPESP: 23/02475-8 - Complexos fosfínicos de Ru(II) com naftoquinonas e derivados: potenciais anticancerígenos, estudos in vitro e in vivo
Beneficiário:Alzir Azevedo Batista
Modalidade de apoio: Auxílio à Pesquisa - Regular