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Ru( ii )–thyminate complexes: new metallodrug candidates against tumor cells

Herein, we used thymine (HThy) as a ligand to form two new ruthenium( ii ) complexes with formula [Ru(PPh 3 ) 2 (Thy)(bipy)]PF 6 ( 1 ) and [Ru(Thy)(bipy)(dppb)]PF 6 ( 2 ). The complexes were characterized by spectroscopic, spectrometric and X-ray crystallography analyses. Complexes 1 and 2 can inter...

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Bibliographic Details
Published in:New journal of chemistry 2018, Vol.42 (9), p.6794-6802
Main Authors: Correa, Rodrigo S., Freire, Vitória, Barbosa, Marília I. F., Bezerra, Daniel P., Bomfim, Larissa M., Moreira, Diogo R. M., Soares, Milena B. P., Ellena, Javier, Batista, Alzir A.
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Language:English
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Summary:Herein, we used thymine (HThy) as a ligand to form two new ruthenium( ii ) complexes with formula [Ru(PPh 3 ) 2 (Thy)(bipy)]PF 6 ( 1 ) and [Ru(Thy)(bipy)(dppb)]PF 6 ( 2 ). The complexes were characterized by spectroscopic, spectrometric and X-ray crystallography analyses. Complexes 1 and 2 can interact with ctDNA presenting binding constants, K b , of 0.4 and 1.2 × 10 3 M −1 , respectively. Their cytotoxic activities towards tumor cell lines (B16-F10, HepG2, K562 and HL-60) and non-tumor cells (PBMCs) were evaluated using the Alamar blue assay. Complex 1 exhibits high cytotoxicity against tumor cells, showing IC 50 values of 0.01 and 1.81 μM against the HL-60 and HepG2 cell lines, respectively. Therefore, compound 1 can be considered as a promising antitumor metallodrug.
ISSN:1144-0546
1369-9261
DOI:10.1039/C7NJ04368F