Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand
| Autor: | Simona Rubino, Luisa Tesoriere, Alessandro Attanzio, Rosa Alduina, Rosalia Busà, Vita Di Stefano, Maria Assunta Girasolo, Santino Orecchio |
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| Přispěvatelé: | Rubino, S., Busà, R., Attanzio, A., Alduina, R., Di Stefano, V., Girasolo, M.A., Orecchio, S., Tesoriere, L. |
| Rok vydání: | 2017 |
| Předmět: |
Stereochemistry
Platinum complex Palladium complex Heterocyclic nitrogen ligand Anticancer activity Antimicrobial activity Clinical Biochemistry Pharmaceutical Science chemistry.chemical_element Platinum Compounds Microbial Sensitivity Tests Ligands 010402 general chemistry 01 natural sciences Biochemistry chemistry.chemical_compound Cell Line Tumor Drug Discovery Escherichia coli Humans Benzothiazoles Molecular Biology 010405 organic chemistry Ligand Spectrum Analysis Organic Chemistry Cell cycle In vitro Anti-Bacterial Agents 0104 chemical sciences Benzothiazole chemistry Settore CHIM/03 - Chimica Generale E Inorganica Molecular Medicine Drug Screening Assays Antitumor Platinum Antibacterial activity Palladium Intracellular |
| Zdroj: | Bioorganic & Medicinal Chemistry. 25:2378-2386 |
| ISSN: | 0968-0896 |
| Popis: | Mono- and binuclear Pt(II) and Pd(II) complexes with 2,20-dithiobis(benzothiazole) (DTBTA) ligand are reported. [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3 (1) and [Pd2(m-Cl)2(DTBTA)2]Cl2 (2) have been synthesized and structurally characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy, MS spectrometry and the content of platinum and palladium was determined using a flame atomic spectrometer. Two different coordination modes of 1 and 2 complexes were found; in both complexes, the coordination of Pt(II) and Pd(II) ions involves the N(3) atoms of the ligand but the binuclear complex 2, is a cis-chloro-bridged palladium complex. Evaluation of their in vitro antitumor activity against two human tumor cell lines human breast cancer (MCF-7) and hepatocellular carcinoma (HepG2); and their antimicrobial activity against Escherichia coli and Kokuria rhizophila was performed. Only complex 1 showed a dose- and time-dependent cytotoxic activity against the two tumor cell lines, associated to apoptosis and accumulation of treated cells in G0/G1 phase of cell cycle, while both 1 and 2 exhibited antimicrobial activity with complex 1 much more potent. The study on intracellular uptake in both MCF-7 and HepG2 cell lines revealed that only platinum of complex 1 is present inside the cells, suggesting a different mode of action of the two compounds. This was also in agreement with the results obtained for the antitumor and antibacterial activity. |
| Databáze: | OpenAIRE |
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