Structural and cytotoxic study of new Pt(II) and Pd(II) complexes with the bi-heterocyclic ligand mepirizole.
Pd(II) and Pt(II) complexes of formulae [MLCl2], where L = mepirizole, were synthesized and characterized. Two complexes were obtained and studied by different techniques: IR, 1H and 13C NMR and XPS spectroscopies and mass spectrometry (electrospray). The crystal structure of the complex cis-dichloro-4-methoxy-2-(5-methoxy-3-methyl- pyrazol-1-yl)-6-methyl-pyrimidinepalladium(II), [Pd(mep)Cl2], was studied by crystal X-ray diffraction. It consists of discrete molecules with planar geometry. Pd(II) ions are four-coordinated by two mepirizole nitrogen atoms (N1 from the pyrazole ring and N4 from the pyrimidine ring) and two chlorine atoms. The geometry of the PdN2Cl2 chromophore is a distortion of the square-planar coordination. Data from powder pattern X-ray diffraction of cis-dichloro-4-methoxy-2-(5-methoxy-3-methyl-pyrazol-1-yl)-6-methyl- pyrimidineplatinum(II), [Pt(mep)Cl2], demonstrated that the two complexes are isostructural. The cytotoxic activity of both Pd and Pt complexes was checked for six different tumor cell lines and was lower than that of cisplatin. The Pt bound to DNA was also checked and only a low percentage is able to cross the cell membrane.
Onoa
G B
GB
Departament de Química Inorgànica, Universitat de Barcelona, Spain.
Moreno
V
V
Font-Bardia
M
M
Solans
X
X
Pérez
J M
JM
Alonso
C
C
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002461:Cell Line, Transformed; D002522:Chlorocebus aethiops; D018360:Crystallography, X-Ray; D004840:Epirizole / Q000737:chemistry* / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D019169:Jurkat Cells; D008024:Ligands; D051379:Mice; D010165:Palladium / Q000737:chemistry*; D010984:Platinum / Q000737:chemistry*; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000970:Antineoplastic Agents; D008024:Ligands; D004840:Epirizole; D010984:Platinum; D010165:Palladium