Title (srp)

Sinteza, karakterizacija i ispitivanje biološke aktivnosti kompleksa bakra(II) sa S,O-tetradentatnim ligandima, derivatima tiosalicilne kiseline

Author

Živanović, Ana S., 1992-

Contributor

Bukonjić, Andriana, 1988-
Radić, Gordana, 1980-
Poljarević, Jelena, 1983-
Mijajlović, Marina, 1987-

Description (eng)

Introduction: The therapeutic application of copper(II)-complexes attracts theattention of researchers due to the possibility of coordination with different donor atoms.Among the ligands that contain sulfur and oxygen in the structure, thiosalicylic acid stands out,whose derivatives show cytotoxicity in tumor therapy.Material and methods: In this Doctoral dissertation, the synthesis of S,O-tetradentateligands, derivatives of thiosalicylic acid and copper(II)-complexes with the mentioned ligandsis described. In order to confirm their structure, various measurements were performed:microanalysis, infrared spectroscopy, nuclear magnetic resonance spectroscopy, electronicparamagnetic resonance and molar conductivity. In order to assess biological activity,nucleophilic substitution reactions of complexes with endogenous ligands (L-methionine, Lcysteine and 5'-GMP), in vitro interactions with ct-DNA (calf thymus DNA) and human serumalbumin (HSA) were performed by absorption spectroscopic analysis and emissionfluorescence, in silico interactions with DNA and HSA. Also, the cytotoxicity of synthesizedligands and complexes on three cell lines was analyzed using MTT colorimetric test.Results: The octahedral geometry of the complex was assumed by the analysis of theperformed measurements. All complexes react to nucleophiles. High values of the bindingconstant indicate that the complexes interact with the DNA molecule and HSA. Interaction witha DNA molecule occurs by intercalation or interaction with a small groove. The complexeshave cytotoxic potential, while the [Cu (S,O-pentylene-thiosalicylic acid)] complex showed thebest cytotoxicity based on IC50 values according to all cell lines.Keywords: S,O-tetradentate ligands, copper(II) complexes, interactions, moleculardocking, antitumor activity

Description (srp)

Uvod: Terapijska primena kompleksa bakra(II) privlači pažnju istraživača zbogmogućnosti koordinovanja sa različitim donorskim atomima. Među liganadima koji ustrukturi sadrže sumpor i kiseonik izdvaja se tiosalicilna kiselina, čiji derivatipokazuju citotoksičnost u terapiji tumora.Materijal i metode: U ovoj Doktorskoj disertaciji opisani su sinteza S,Otetradentatnih liganada, derivata tiosalicilne kiseline i kompleksa bakra(II) sanavedenim ligandima. Radi potvrde njihove strukture, sprovedena su različita merenja:mikroanaliza, infracrvena spektroskopija, nuklearno-magnetno-rezonancionaspektroskopija, elektronska paramagnetna rezonancija i molarna provodljivost. Ucilju procene biološke aktivnosti sprovedene su nukleofilne supstitucionereakcije kompleksa sa endogenim ligandima (L-metioninom, L-cisteinom i 5’-GMP), invitro interakcije sa ST-DNK (eng. calf thymus, DNK timusa govečeta) i humanimserumskim albuminom (HSA) pomoću apsorpcione spektroskopske analize i emisionefluorescencije, in silico interakcije sa DNK i HSA. Takođe, primenom MTTkolorimetrijskog testa analizirana je citotoksičnost sintetisanih liganada ikompleksa na tri ćelijske linije.Rezultati: Analizom sprovedenih merenja pretpostavljena je oktaedarskageometrija kompleksa. Svi kompleksi podležu reakcijama nukleofilne supstitucije.Visoke vrednosti konstante vezivanja pokazuju da kompleksi interaguju sa molekulomDNK i HSA. Interakcija sa DNK molekulom dešava se interkalacijom iliinterakcijom sa malim žlebom. Kompleksi imaju citotoksični potencijal, dok je premasvim ćelijskim linijama najbolju citotoksičnost na osnovu IC50 vrednosti pokazaokompleks [Cu(S,O-pentilen-tiosalicilna kiselina)].

Description (srp)

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Object languages

Serbian

Date

2022

Rights

Creative Commons License
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CC BY-NC-SA 3.0 AT - Creative Commons Attribution-NonCommercial-ShareAlike 3.0 Austria License.

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