Ethacrynic acid is a broad acting glutathione transferase inhibitor, and its incorporation within suitable metal complexes results in enhancement of the anticancer activity.1 A series of pyridine- and phosphine-based ligands functionalized with ethacrynic acid were synthesized and coordinated to ruthenium(II)-arene complexes. All the compounds (ligands and complexes) were fully characterized by different analytical and spectroscopic techniques and, in some cases, by single-crystal X-ray diffraction. The in vitro anticancer activity of the compounds was studied towards two different tumour cell lines, the compounds displaying moderate antiproliferative activity.2 The interactions with two well-known model proteins were analysed through ESI MS spectrometry and the resulting metallodrug–protein adducts identified.

Arene Ruthenium Complexes with Ethacrynic Acid-Modified Ligands: Synthesis, Characterization and Antiproliferative Activity

AGONIGI, GABRIELE;BIANCALANA, LORENZO;CHIELLINI, FEDERICA;FUNAIOLI, TIZIANA;GABBIANI, CHIARA;MARCHETTI, FABIO;PAMPALONI, GUIDO;
2016

Abstract

Ethacrynic acid is a broad acting glutathione transferase inhibitor, and its incorporation within suitable metal complexes results in enhancement of the anticancer activity.1 A series of pyridine- and phosphine-based ligands functionalized with ethacrynic acid were synthesized and coordinated to ruthenium(II)-arene complexes. All the compounds (ligands and complexes) were fully characterized by different analytical and spectroscopic techniques and, in some cases, by single-crystal X-ray diffraction. The in vitro anticancer activity of the compounds was studied towards two different tumour cell lines, the compounds displaying moderate antiproliferative activity.2 The interactions with two well-known model proteins were analysed through ESI MS spectrometry and the resulting metallodrug–protein adducts identified.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/806633
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact