Cytotoxic gold(iii) complexes incorporating a 2,2':6',2''-terpyridine ligand framework - the impact of the substituent in the 4'-position of a terpy ring

K Czerwińska; M Golec; M Skonieczna; J Palion-Gazda; D Zygadło; A Szlapa-Kula; S Krompiec; B Machura; A Szurko

doi:10.1039/c6dt04584g

Cytotoxic gold(iii) complexes incorporating a 2,2':6',2''-terpyridine ligand framework - the impact of the substituent in the 4'-position of a terpy ring

Dalton Trans. 2017 Mar 7;46(10):3381-3392. doi: 10.1039/c6dt04584g.

Authors

K Czerwińska¹, M Golec², M Skonieczna³, J Palion-Gazda¹, D Zygadło², A Szlapa-Kula⁴, S Krompiec⁴, B Machura¹, A Szurko²

Affiliations

¹ Department of Crystallography, Institute of Chemistry, University of Silesia, 9th Szkolna St, 40-006 Katowice, Poland. bmachura@poczta.onet.pl.
² August Chełkowski Institute of Physics, University of Silesia, Uniwersytecka 4, 40-007 Katowice, Poland and Silesia Center for Education and Interdisciplinary Research, 75 Pułku Piechoty 1A, 41-500 Chorzów, Poland. agnieszka.szurko@us.edu.pl.
³ Silesian University of Technology, Center Biotechnology Bioengineering and Bioinformatics, Gliwice, Poland and Silesian University of Technology, Institute of Automatic Control, Gliwice, Poland.
⁴ Department of Inorganic, Organometallic Chemistry and Catalysis, Institute of Chemistry, University of Silesia, 9th Szkolna St., 40-006 Katowice, Poland.

PMID: 28234396
DOI: 10.1039/c6dt04584g

Abstract

Two gold(iii) complexes incorporating 2,2':6',2''-terpyridine derivatives have been synthesised and characterized, and the possibility of tuning the cytotoxic activity by structural modifications of a terpy ligand has been examined. Both complexes [AuCl(4'-R¹-terpy)](PF₆)₂ (1) and [AuCl(4'-R²-terpy)](PF₆)₂ (2), where R¹ is 2-pyridyl and R² is 3-pyridyl, show good anti-proliferative activities against HCT116, which are higher in relation to those of the free ligands, [AuCl(terpy)](PF₆)₂ and standard anticancer drug cisplatin. The cytotoxic properties of the gold complexes were examined by MTS assay, cell cycle and apoptosis analysis, ROS measurements, determination of mitochondrial membrane potential and mass, and staining of phosphatidylserine with Annexin-V antibody FITC-conjugated together with PI.