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Ruthenium(II)/(III) complexes of 4-hydroxy-pyridine-2,6-dicarboxylic acid with PPh sub(3)/AsPh sub(3) as co-ligand: Impact of oxidation state and co-ligands on anticancer activity in vitro

With the aim to develop more efficient, less toxic, target specific metal drugs and evaluate their anticancer properties in terms of oxidation state and co-ligand sphere, a sequence of Ru super(II), Ru super(III) complexes bearing 4-hydroxy-pyridine-2,6-dicarboxylic acid and PPh sub(3)/AsPh sub(3) w...

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Published in:Dalton transactions : an international journal of inorganic chemistry 2012-01, Vol.41 (7), p.2066-2077
Main Authors: Kamatchi, Thangavel Sathiya, Chitrapriya, Nataraj, Lee, Hyosun, Fronczek, Chris F, Fronczek, Frank R, Natarajan, Karuppannan
Format: Article
Language:English
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Summary:With the aim to develop more efficient, less toxic, target specific metal drugs and evaluate their anticancer properties in terms of oxidation state and co-ligand sphere, a sequence of Ru super(II), Ru super(III) complexes bearing 4-hydroxy-pyridine-2,6-dicarboxylic acid and PPh sub(3)/AsPh sub(3) were synthesized and structurally characterized. Biological studies such as DNA binding, antioxidant assays and cytotoxic activity were carried out and their anticancer activities were evaluated. Interactions of the complexes with calf thymus DNA revealed that the triphenylphosphine complexes could bind more strongly than the triphenylarsine complexes. The free radical scavenging ability, assessed by a series of in vitro antioxidant assays involving DPPH radical, hydroxyl radical, nitric oxide radical, superoxide anion radical, hydrogen peroxide and metal chelating assay, showed that the Ru super(III) complexes possess excellent radical scavenging properties compared to those of Ru super(II). Cytotoxicity studies using three cancer lines viz HeLa, HepG2, HEp-2 and a normal cell line NIH 3T3 showed that Ru super(II) complexes exhibited substantial cytotoxic specificity towards cancer cells. Furthermore, the Ru super(II) complexes were found to be superior to Ru super(III) complexes in inhibiting the growth of cancer cells.
ISSN:1477-9226
1477-9234
DOI:10.1039/c1dt11273b