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J Inorg Biochem ; 102(1): 33-45, 2008 Jan.
Article in English | MEDLINE | ID: mdl-17689616

ABSTRACT

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.


Subject(s)
Antineoplastic Agents/chemistry , Organoplatinum Compounds/chemistry , Palladium/chemistry , Pyrazolones/chemistry , Pyrazolones/therapeutic use , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Female , Humans , Hydrogen Bonding , Molecular Structure , Organoplatinum Compounds/chemical synthesis , Ovarian Neoplasms/drug therapy , Pyrazolones/chemical synthesis , X-Ray Diffraction
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