Ru(II)-based complexes with N-(acyl)-N',N'-(disubstituted)thiourea ligands: Synthesis, characterization, BSA- and DNA-binding studies of new cytotoxic agents against lung and prostate tumour cells.

Four ruthenium(II)-based complexes with N-(acyl)-N',N'-(disubstituted)thiourea derivatives (Th) were obtained. The compounds, with the general formula trans-[Ru(PPh3)2(Th)(bipy)]PF6, interact with bovine serum albumin (BSA) and DNA.

BSA-binding constants, which were in the range of 3 3-6 5×10(4)M(-1), and the thermodynamic parameters (ΔG, ΔH and ΔS), suggest spontaneous interactions with this protein by electrostatic forces due to the positive charge of the complexes Also, binding constant by spectrophotometric DNA titration (Kb=0 8-1 8×10(4)M(-1)) and viscosity studies indicate weak interactions between the complexes and DNA Cytotoxicity assays against DU-145 (prostate cancer) and A549 (lung cancer) tumour cells revealed that the complexes are more active in tumour cells than in normal (L929) cells, and that they present high cytotoxicity (low IC50 values) compared with the reference metallodrug, cisplatin

Journal of inorganic biochemistry 2015 Apr 22 [Epub ahead of print]

Rodrigo S Correa, Katia M de Oliveira, Fábio G Delolo, Anislay Alvarez, Raúl Mocelo, Ana M Plutin, Marcia R Cominetti, Eduardo E Castellano, Alzir A Batista

Departamento de Química, Universidade Federal de São Carlos, UFSCar, Rodovia Washington Luís KM 235, CP 676, 13561-901, São Carlos, SP, Brazil Electronic address: rodricorrea@ufscar br , Departamento de Química, Universidade Federal de São Carlos, UFSCar, Rodovia Washington Luís KM 235, CP 676, 13561-901, São Carlos, SP, Brazil , Departamento de Química, Universidade Federal de São Carlos, UFSCar, Rodovia Washington Luís KM 235, CP 676, 13561-901, São Carlos, SP, Brazil , Laboratório de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, Habana 10400, Cuba , Laboratório de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, Habana 10400, Cuba , Laboratório de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, Habana 10400, Cuba , Departamento de Gerontologia, Universidade Federal de São Carlos, São Carlos, SP, Brazil , Departamento de Física e Informática, Instituto de Física de São Carlos, Universidade de São Paulo, CP 369, 13560-970, São Carlos, SP, Brazil , Departamento de Química, Universidade Federal de São Carlos, UFSCar, Rodovia Washington Luís KM 235, CP 676, 13561-901, São Carlos, SP, Brazil  

PubMed

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