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Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand
- Source :
- Bioorganic & Medicinal Chemistry. 25:2378-2386
- Publication Year :
- 2017
- Publisher :
- Elsevier BV, 2017.
-
Abstract
- 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.
- Subjects :
- 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
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....52e798bbfc610ef75264e9e770e3e566