Getreuer, Paul and Marretta, Laura and Toyoglu, Emine and Dömötör, Orsolya and Hejl, Michaela and Prado-Roller, Alexander and Cseh, Klaudia and Legin, Anton A. and Jakupec, Michael A. and Barone, Giampaolo and Terenzi, Alessio and Keppler, Bernhard K. and Kandioller, Wolfgang (2024) Investigating the anticancer potential of 4-phenylthiazole derived Ru(II) and Os(II) metalacycles. DALTON TRANSACTIONS. ISSN 1477-9226
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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 H-1-, C-13- 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.
| Item Type: | Article |
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| Additional Information: | Funding Agency and Grant Number: University of Vienna; Doctoral School of Chemistry; Universita Degli Studi di Palermo; Development and Innovation Office-NKFIA (Hungary) [TKP-2021-EGA-32] Funding text: We thank the University of Vienna, the Doctoral School of Chemistry and Universita Degli Studi di Palermo for financial support. We also thank the Centre for X-Ray Structure Analysis (University of Vienna) for determination of the crystal structures, the NMR Centre (University of Vienna) for 2D NMR spectra and the Mass Spectrometry Centre (University of Vienna) for measurement of the MS-spectra. O.D. gratefully acknowledges the financial support from TKP-2021-EGA-32 project of the Development and Innovation Office-NKFIA (Hungary). Finally, we thank AteN Center (University of Palermo) for FRET melting measurements. |
| Uncontrolled Keywords: | IN-VITRO; DRUG; STABILITY; RUTHENIUM(II) ARENE COMPLEXES; ORGANOMETALLIC COMPLEXES; OSMIUM(II); antitumor; METAL-COMPOUNDS; |
| Subjects: | Q Science / természettudomány > QD Chemistry / kémia |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 31 May 2024 06:31 |
| Last Modified: | 31 May 2024 06:31 |
| URI: | https://real.mtak.hu/id/eprint/196193 |
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