Investigation of the cytotoxic potential of methyl imidazole-derived thiosemicarbazones and their copper(ii) complexes with dichloroacetate as a co-ligand
| Main Authors: | Palamarciuc Oleg, Milunović Miljan NM, Sirbu Angela, Stratulat Elena, Pui Aurel, Gligorijević Nevenka, Radulović Siniša, Kožišek Jozef, Darvasiova Denisa, Rapta Peter, Enedy Eva A, Novitchi Ghenadie, Shova Sergiu, Arion Vladimir B |
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| Format: | Article Journal |
| Bahasa: | eng |
| Terbitan: |
, 2019
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| Subjects: | |
| Online Access: |
https://zenodo.org/record/4323158 |
Daftar Isi:
- A series of six imidazole-derived thiosemicarbazones (HL1–HL6) and their copper(II) complexes (1–6)were synthesised and characterised by analytical, spectroscopic, electrochemical and single crystal X-raydiffraction techniques. In addition, solution studies and the results of antiproliferative activity in human cancer cell lines with some insights into the mechanism of cancer cell death are also reported. In particular, the substitution of one hydrogen at the terminal N-atomof the thiosemicarbazide moiety by a phenyl group resulted in slightly enhanced antiproliferative activity.HL3andHL6showed lower IC50values comparedtoHL1andHL4in MDA-MB-453 and LS174 cancer cell lines. The copper(II) complexes3and6exhibit a2.4- and 4.7-fold increase of activity compared to parent proligands in MDA-MB-453 cancer cell line,respectively. The complex formation of the proligands with copper(II) increased their antiproliferative activity in all investigated cell lines. The cell cycle perturbations, apoptotic potential and the analysis of morphological changes in the A549 cell line induced by3and6revealed cytostatic rather than cytotoxic effect
- Supplementary information http://www.rsc.org/suppdata/c8/nj/c8nj04041a/c8nj04041a1.pdf The article was funded by: V. B. A. to the FWF (Austrian Science Fund) for the grant no. P28223-N34. This study was also financially supported by Research and Development Agency of the Slovak Republic under the contracts no. APVV-15-0053 and APVV-15-0079 and Scientific Grant Agency of the Slovak Republic (VEGA Projects 1/0871/16, 1/0416/17 and 1/0466/18), the Ministry of Education, Science, Research and Sport of the Slovak Republic within the Research and Development Operational Programme for the project ''University Science Park of STU Bratislava'', ITMS 26240220084, co-funded by the European Regional Development Fund. This work was also supported by Serbian Ministry of Education, Science and Technology, Grant III41026 and Hungarian National Research Development and Innovation Office through the project FK 12420 and the UNKP-17-4 New National Excellence Program of the Ministry of Human Capacities. O. P., A. S. and E. S. thank AUF (Agence Universitaire de la Francophonie) for funding the project no. 15.817.02.28F