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

The synthesis and chemical characterization of three new transplatinum complexes of structural formula trans-[PtCl(2)(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 V...

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Bibliographic Details
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
Subjects:
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Biological and medical sciences
Cell Line, Transformed
Cercopithecus aethiops
Cisplatin - pharmacology
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
General aspects
Genes, ras
HeLa Cells
Humans
Inhibitory Concentration 50
Jurkat Cells
Medical sciences
Organoplatinum Compounds - chemical synthesis
Organoplatinum Compounds - chemistry
Organoplatinum Compounds - pharmacology
Pharmacology. Drug treatments
Tumor Cells, Cultured
Vero Cells
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Summary:The synthesis and chemical characterization of three new transplatinum complexes of structural formula trans-[PtCl(2)(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-PtCl(2) 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