Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand

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RESEARCH PRODUCT

Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand

Simona Rubino Luisa Tesoriere Alessandro Attanzio Rosa Alduina Rosalia Busà Vita Di Stefano Maria Assunta Girasolo Santino Orecchio

subject

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 Palladium

description

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.

year	journal	country	edition	language
2017-04-01	Bioorganic & Medicinal Chemistry

https://doi.org/10.1016/j.bmc.2017.02.067