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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.)

DNA binding, topoisomerase inhibition and cytotoxicity of palladium(II) complexes with 1,10-phenanthroline and thioureas

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Author(s):
Barra, Carolina V. [1, 2] ; Rocha, Fillipe V. [3] ; Morel, Laurent [4] ; Gautier, Arnaud [5] ; Garrido, Saulo S. [6] ; Mauro, Antonio E. [1] ; Frem, Regina C. G. [1] ; Netto, Adelino V. G. [1]
Total Authors: 8
Affiliation:
[1] UNESP, Inst Quim, Dept Quim Geral & Inorgan, BR-14801970 Araraquara, SP - Brazil
[2] Inst Fed Educ Ciencia & Tecnol, BR-14801600 Araraquara, SP - Brazil
[3] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Clermont Ferrand, Clermont Univ, GreD UMR CNRS 6247, INSERM U931, 24 Ave Landais, F-63177 Aubiere - France
[5] Univ Clermont Ferrand, Clermont Univ, ICCF, CNRS, UMR 6296, F-63177 Aubiere - France
[6] UNESP, Inst Quim, Dept Bioquim & Tecnol Quim, BR-14801970 Araraquara, SP - Brazil
Total Affiliations: 6
Document type: Journal article
Source: Inorganica Chimica Acta; v. 446, p. 54-60, MAY 1 2016.
Web of Science Citations: 18
Abstract

Metallointercalators represent a promising alternative in cancer chemotherapy. We present herein DNA binding, topoisomerase inhibition and cytotoxic studies on a series of complexes of general formulae {[}Pd (phen)(tu{*})(2)](2+) incorporating the intercalator 1,10-phenanthroline and thiourea ligands (L = thiourea 1, N-methylthiourea 2, N,N'-dimethylthiourea 3). DNA-unwinding results showed that the complexes can induce the unwinding of the plasmid DNA. The binding constants (K-b) for the interaction of the complexes with SS-DNA were determined by UV spectroscopy. Competitive experiments with ethidium bromide (EB) were investigated by fluorescence spectroscopy and show that all the complexes were able to displace EB from the DNA-EB complex. The results suggest that they may interact with DNA by intercalation. Compounds were tested against human oral carcinoma cell line (KB), human breast cancer cell line (MCF7) and cisplatin-resistant human breast cancer cell line (MCF7-R) and showed good cytotoxic activity towards MCF7-R. Compounds 2 and 3 were also able to cause topo II inhibition. (C) 2016 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 14/11340-0 - NEW Pd(II) ORGANOMETALLIC COMPLEXES: INVESTIGATION OF THEIR POTENTIAL AS CATHEPSIN B INHIBITORS
Grantee:Carolina Valério Barra Rocha
Support Opportunities: Scholarships in Brazil - Post-Doctoral