Please use this identifier to cite or link to this item:
https://dipositint.ub.edu/dspace/handle/2445/49383
Title: | Platinum (II) and palladium (II) complexes with (N,N') and (C,N,N') ligands derived from pyrazole as anticancer and antimalarial agents: synthesis, characterization and in vitro activities |
Author: | Quirante Serrano, Josefina Ruiz, Daniel González Gazulla, Asensio López Martínez, Ma. Concepción Cascante i Serratosa, Marta Cortés Giràldez, Roldàn Messeguer i Peypoch, Ramon Calvis, Carme Baldomà Llavinés, Laura Pradines, Bruno Pascal, Aurélie Guérardel, Yann Font Bardia, Ma. Mercedes Calvet Pallàs, Maria Teresa Biot, Christophe |
Keywords: | Càncer Malària Pal·ladi (Element químic) Platí Cancer Malaria Palladium Platinum |
Issue Date: | 2011 |
Publisher: | Elsevier B.V. |
Abstract: | The study of the reactivity of three 1-(2-dimethylaminoethyl)-1H-pyrazole derivatives of general formula [1-(CH2)2NMe2}-3,5-R2-pzol] {where pzol represents pyrazole and Rdouble bond; length as m-dashH (1a), Me (1b) or Ph (1c)} with [MCl2(DMSO)2] (Mdouble bond; length as m-dashPt or Pd) under different experimental conditions allowed us to isolate and characterize cis-[M{κ2-N,N′-{[1-(CH2)2NMe2}-3,5-R2-pzol])}Cl2] {MMdouble bond; length as m-dashPtPt (2a-2c) or Pd (3a-3c)} and two cyclometallated complexes [M{κ3-C,N,N′-{[1-(CH2)2NMe2}-3-(C5H4)-5-Ph-pzol])}Cl] {Mdouble bond; length as m-dashPt(II) (4c) or Pd(II) (5c)}. Compounds 4c and 5c arise from the orthometallation of the 3-phenyl ring of ligand 1c. Complex 2a has been further characterized by X-ray crystallography. Ligands and complexes were evaluated for their in vitro antimalarial against Plasmodium falciparum and cytotoxic activities against lung (A549) and breast (MDA MB231 and MCF7) cancer cellular lines. Complexes 2a-2c and 5c exhibited only moderate antimalarial activities against two P. falciparum strains (3D7 and W2). Interestingly, cytotoxicity assays revealed that the platinacycle 4c exhibits a higher toxicity than cisplatin in the three human cell lines and that the complex 2a presents a remarkable cytotoxicity and selectivity in lung (IC50 = 3 μM) versus breast cancer cell lines (IC50 > 20 μM). Thus, complexes 2c and 4c appear to be promising leads, creating a novel family of anticancer agents. Electrophoretic DNA migration studies in presence of the synthesized compounds have been performed, in order to get further insights into their mechanism of action. |
Note: | Versió postprint del document publicat a: http://dx.doi.org/10.1016/j.jinorgbio.2011.09.021 |
It is part of: | Journal of Inorganic Biochemistry, 2011, vol. 105, num. 12, p. 1720-1728 |
URI: | http://hdl.handle.net/2445/49383 |
Related resource: | http://dx.doi.org/10.1016/j.jinorgbio.2011.09.021 |
ISSN: | 0162-0134 |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
598960.pdf | 647.63 kB | Adobe PDF | View/Open |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.