Investigating the anticancer potential of 4-phenylthiazole derived Ru(ii) and Os(ii) metalacycles

Author(s): Paul Getreuer, Laura Marretta, Emine Toyoglu, Orsolya Dömötör, Michaela Hejl, Alexander Prado-Roller, Klaudia Cseh, Anton A. Legin, Michael A. Jakupec, Giampaolo Barone, Alessio Terenzi, Bernhard K. Keppler, Wolfgang Kandioller
Abstract: In this contribution we report the synthesis, characterization and in vitro anticancer activity of novel cyclometalated 4-phenylthiazole-derived ruthenium(ii) (2a-e) and osmium(ii) (3a-e) complexes. Formation and sufficient purity of the complexes were unambigiously confirmed by ¹H-, ¹³C- and 2D-NMR techniques, X-ray diffractometry, HRMS and elemental analysis. The binding preferences of these cyclometalates to selected amino acids and to DNA models including G-quadruplex structures were analyzed. Additionally, their stability and behaviour in aqueous solutions was determined by UV-Vis spectroscopy. Their cellular accumulation, their ability of inducing apoptosis, as well as their interference in the cell cycle were studied in SW480 colon cancer cells. The anticancer potencies were investigated in three human cancer cell lines and revealed IC₅₀ values in the low micromolar range, in contrast to the biologically inactive ligands.
Organisation(s): Department of Inorganic Chemistry, Core Facility Crystal Structure Analysis
External organisation(s): Vienna Doctoral School in Chemistry (DoSChem), Università degli Studi di Palermo, University of Szeged, Research Cluster Translational Cancer Therapy Research
Journal: Dalton Transactions
Volume: 53
Pages: 5567-5579
No. of pages: 13
ISSN: 1477-9226
DOI: https://doi.org/10.1039/d4dt00245h
Publication date: 03-2024
Peer reviewed: Yes
Austrian Fields of Science 2012: 104003 Inorganic chemistry, 301904 Cancer research
ASJC Scopus subject areas: Inorganic Chemistry
Sustainable Development Goals: SDG 3 - Good Health and Well-being
Portal url: https://ucrisportal.univie.ac.at/en/publications/7d354a0f-f066-4862-a393-1c1ad3085300