Preparation and Characterization of Novel trans-[PtCl2(amine)(isopropylamine)] Compounds:  Cytotoxic Activity and Apoptosis Induction in r as-Transformed Cells

The synthesis and chemical characterization of three new transplatinum complexes of structural formula trans-[PtCl2(amine)(isopropylamine)] (amine = n,n-dimethylamine, propylamine, and butylamine), 1−3, are described. Cytotoxicity tests in tumor cell lines sensitive to cis-DDP (Jurkat, Hela, and Ver...

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Published in:Journal of medicinal chemistry 1999-10, Vol.42 (20), p.4264-4268
Main Authors: Montero, Eva I, Díaz, Sonia, González-Vadillo, Ana Ma, Pérez, José M, Alonso, C, Navarro-Ranninger, Carmen
Format: Article
Language:English
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Summary:The synthesis and chemical characterization of three new transplatinum complexes of structural formula trans-[PtCl2(amine)(isopropylamine)] (amine = n,n-dimethylamine, propylamine, and butylamine), 1−3, are described. Cytotoxicity tests in tumor cell lines sensitive to cis-DDP (Jurkat, Hela, and Vero) and also in tumor cell lines overexpressing ras oncogenes and resistant to cis-DDP (HL-60 and Pam 212-ras) show that complexes 1 and 3 have higher cytotoxic activity than cisplatin. Moreover, these two trans-Pt(II) complexes kill Pam 212-ras cells through apoptosis induction. These results suggest that trans-PtCl2 complexes with asymmetric aliphatic amines may be considered a new class of biologically active trans-platinum drugs.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm991015e