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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Correa, Rodrigo S. [1] ; de Oliveira, Katia M. [1] ; Delolo, Fabio G. [1] ; Alvarez, Anislay [2] ; Mocelo, Raul [2] ; Plutin, Ana M. [2] ; Cominetti, Marcia R. [3] ; Castellano, Eduardo E. [4] ; Batista, Alzir A. [1]
Total Authors: 9
[1] Univ Fed Sao Carlos, Dept Quim, BR-13561901 Sao Carlos, SP - Brazil
[2] Univ La Habana, Fac Quim, Lab Sintesis Organ, Havana 10400 - Cuba
[3] Univ Fed Sao Carlos, Dept Gerontol, BR-13561901 Sao Carlos, SP - Brazil
[4] Univ Sao Paulo, Inst Fis Sao Carlos, Dept Fis & Informat, BR-13560970 Sao Carlos, SP - Brazil
Total Affiliations: 4
Document type: Journal article
Source: Journal of Inorganic Biochemistry; v. 150, p. 63-71, SEP 2015.
Web of Science Citations: 44

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 x 10(4) M-1, and the thermodynamic parameters (Delta G, Delta H and Delta S), 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 x 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. (C) 2015 Published by Elsevier Inc. (AU)

FAPESP's process: 13/26559-4 - Structural modifications in biologically active Ru(II) complexes toward the design of new metallodrug candidates
Grantee:Rodrigo de Souza Corrêa
Support type: Scholarships in Brazil - Post-Doctorate
FAPESP's process: 14/04147-9 - Evaluation of anticancer properties of ruthenium(II)complexes containing lapachol and lawsone bioligands
Grantee:Katia Mara de Oliveira
Support type: Scholarships in Brazil - Doctorate