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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
Pal·ladi (Element químic)
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:
It is part of: Journal of Inorganic Biochemistry, 2011, vol. 105, num. 12, p. 1720-1728
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ISSN: 0162-0134
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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