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Sinteza, karakterizacija i potencijalna biološka aktivnost binuklearnih kompleksa bakra(II) sa S-alkil derivatima tiosalicilne kiseline

Synthesis, characterization and potential TI biological activity of binuclear copper(II)- complexes with S-alkyl derivatives of thiosalicylic acid

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Author
Nikolić, Miloš V.
Mentor
Radić, Gordana P.
Committee members
Arsenijević, Nebojša
Sabo, Tibor
Jevtić, Verica
Milovanović, Мarija
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Abstract
U ovoj doktorskoj disertaciji opisane su sinteze S-alkil derivata tiosalicilne kiseline i odgovarajućih binuklearnih kompleksa bakra(II). Sastav nagrađenih jedinjenja potvrđen je na osnovu rezultata elementalne mikroanalize. Struktura sintetisanih jedinjenja pretpostavljena je na osnovu rezultata infracrvene spektroskopije i magnetnih merenja, dok je stvarna struktura dobijenih jedinjenja određena na osnovu rendgenske strukturne analize kompleksa pri čemu je utvrđena binuklearna struktura kompleksa. Citotoksični efekat svih ispitivanih jedinjenja bio je snažniji prema HCT-116 ćelijskoj liniji u poređenju sa efektom prema CT26 i CT26.CL25 ćelijskim linijama. Citotoksična aktivnost novosintetisanih kompleksa bakra prema CT26 i CT26.CL25 ćelijskim linijama bila je značajno slabija u poređenju sa aktivnošću koju ostvaruje cisplatina. Svi testirani komleksi pokazali su umerenu i selektivnu antibakterijsku kao i slabu antigljivičnu aktivnost. Poredeći dobijene rezultate sa rezultatima poziti...vne kontrole može se zaključiti da ispitivana jedinjenja pokazuju nisku antibiofilm aktivnost. Izuzeci su primećeni kod bakterija Staphylococcus aureus i Pseudomonas aeruginosa. Antioksidativna aktivnost ispitivanih kompleksa nije bila značajna. Otkriće potencijalne biološke aktivnosti kompleksa bakra(II) uslovilo bi povećano interesovanje za dalja istraživanja u oblasti koordinacije jona bakra sa farmakološki aktivnim ligandima u cilju postizanja snažnijeg biološkog efekta kompleksa čime bi se dao značajan doprinos u potrazi za novim i efikasnijim antibakterijskim, antigljivičnim i antitumorskim lekovima.

In this doctoral thesis the synthesis of S-alkyl derivatives of thiosalicylic acid and corresponding binuclear copper(II)-complexes are described. The composition of obtained compounds are proposed on the basis of elemental microanalysis. The structure of the synthesized compounds are proposed on the basis of infrared spectra and magnetic measurements, while the real structure of the obtained compounds was determined on the basis of X-ray analysis, whereby the binuclear structure of the complexes has been shown. Cytotoxic effect of all the tested compounds was stronger on HCT-116 cell line compared to CT26 and CT26.CL25 cell lines. Cytotoxic activity of new copper(II)-complexes on murine cell lines CT26 and CT26.CL25 was significantly lower compared to activity of cisplatin. All the tested complexes demonstrated moderate or selective antibacterial activity and low antifungal activity. Comparing the results with the results of the positive control it can be concluded that the tested com...plexes generally showed lower antibiofilm activity. The exceptions are observed in bacteria Staphylococcus aureus and Pseudomonas aeruginosa. Antioxidant activity of tested complexes was not significant.The discovery of the potential biological activity of copper(II)-complexes would increase the interest for further research in the field of coordination of copper ions with pharmacologically active ligands in order to achieve a stronger biological effect of the complexes which would give a significant contribution to the search for new and more effective antibacterial, antifungal and anticancer drugs.

Faculty:
Универзитет у Крагујевцу, Факултет медицинских наука
Date:
26-12-2016
[ Google Scholar ]
Handle
https://hdl.handle.net/21.15107/rcub_nardus_7680
URI
https://nardus.mpn.gov.rs/handle/123456789/7680
http://eteze.kg.ac.rs/application/showtheses?thesesId=4637
https://fedorakg.kg.ac.rs/fedora/get/o:763/bdef:Content/download

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