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Palladium(II) compounds of putrescine and spermine. Synthesis, characterization, and DNA-binding and antitumor properties

1993; Elsevier BV; Volume: 52; Issue: 1 Linguagem: Inglês

10.1016/0162-0134(93)85621-e

1873-3344

Carmen Navarro‐Ranninger, Félix Zamora, J.R. Masaguer, J.M. González-Pérez, Vı́ctor M. González, C. Alonso,

Synthesis and Biological Evaluation

The reaction of putrescine (Put) with K2PdCl4 and PdCl2 resulted in the synthesis of compounds of formula [PutH2][PdCl4] and [Pd2Cl4(Put)2]. Compounds of formula [PdCl2(SpermH2)][PdCl4] and [Pd2Cl4(Sperm)] have been also synthesized by reaction of spermine (Sperm) with K2PdCl4. The structure of all these compounds has been analyzed by IR and 1H NMR. UV and CD spectroscopic data have shown that all the Pd(II)-polyamine compounds synthesized induce conformational changes in the circular forms of plasmid DNA. Determinations by electrophoresis in agarose gels of the mobility of the DNA in drug:DNA complexes indicated that only the Pdd(II)-putrescine compounds have the ability to induce significant conformational changes in the covalently closed circular (ccc) form of the pUC8 plasmid DNA. The Pdd(II)-putrescine and Pdd(II)-spermine compounds were also assayed for in vitro antiproliferative activity against MDA-MB 468 and HL-60 human cancer cells. The results suggest that the putrescine complexes may be regarded as potential antitumor agents because the ID50 value of all of the Pdd(II)-putrescine complexes is twofold lower than the ID50 of cis-DDP. Our data also show that, on the other hand, the Pdd(II)-spermine compounds have low antiproliferative activity.