N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies

Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we repo...

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Detalles Bibliográficos
Autores: Lenis Rojas, Oscar A., Cordeiro, Sandra, Horta Meireles, Marta, Fernández, Jhonathan Angel Araujo, Vila, Sabela Fernández, Rubiolo, Juan Andrés, Cabezas Sainz, Pablo, Sanchez, Laura, Fernandes, Alexandra R., Royo, Beatriz
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2021
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/153537
Acceso en línea:http://hdl.handle.net/11336/153537
Access Level:acceso abierto
Palabra clave:ANTICANCER ACTIVITY
IRON(II)–NHC COMPLEXES
N-HETEROCYCLIC CARBENE
ZEBRAFISH
https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
Descripción
Sumario:Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.

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