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 comp lexes of structural formula trans-[PtCl2(amine)(isopropylamine)] (amine = n ,n-dimethylamine, propylamine, and butylamine), 1-3, are described. Cytotox icity tests in tumor cell lines sensitive to cis-DDP (Jurkat, Hela, and Ver o) 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) complex es kill Pam 212-ras cells through apoptosis induction. These results sugges t that trans-PtCl2 complexes with asymmetric aliphatic amines may be consid ered a new class of biologically active trans-platinum drugs.