New Pd(II) and Pt(II) complexes with N,S-chelated pyrazolonate ligands: molecular and supramolecular structure and preliminary study of their in vitro antitumoral activity.
New Pd(II) and Pt(II) complexes [ML2] (HL=a substituted 2,5-dihydro-5-oxo-1H-pyrazolone-1-carbothioamide) have been synthesized by reacting K2MCl4 (M=Pd, Pt) or Pd(OAc)2 with beta-ketoester thiosemicarbazones. The structures of seven of these complexes were determined by X-ray diffraction. Although all exhibit a distorted square-planar coordination with trans- or (in one case) cis-[MN2S2] kernels, their supramolecular arrangements vary widely from isolated molecules to 3D-networks. The in vitro antitumoral assays performed with two HL ligands and their metal complexes showed significant cytostatic activity for the latter, with the most active [ML2] derivative (a palladium complex) being about sixteen times more active than cis-DDP against the cisplatinum-resistant cell line A2780cisR.
Casas
José S
JS
Departamento de Química Inorgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Galicia, Spain. qiscasas@usc.es
Castellano
Eduardo E
EE
Ellena
Javier
J
García-Tasende
María S
MS
Pérez-Parallé
M Luz
ML
Sánchez
Agustín
A
Sánchez-González
Angeles
A
Sordo
José
J
Touceda
Angeles
A
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D006860:Hydrogen Bonding; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D010051:Ovarian Neoplasms / Q000188:drug therapy; D010165:Palladium / Q000737:chemistry*; D047069:Pyrazolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; D047069:Pyrazolones; D010165:Palladium