title: Preparation and characterization of novel trans-[PtCl(2)(amine)(isopropylamine)] compounds: cytotoxic activity and apoptosis induction in ras-transformed cells.
abstract: 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.
authors.affiliation: Departamento de Química Inorgánica, Universidad Autónoma de Madrid, 28049 Madrid, Spain.
authors.forename: E I
authors.initials: EI
authors.lastname: Montero
authors.forename: S
authors.initials: S
authors.lastname: Díaz
authors.forename: A M
authors.initials: AM
authors.lastname: González-Vadillo
authors.forename: J M
authors.initials: JM
authors.lastname: Pérez
authors.forename: C
authors.initials: C
authors.lastname: Alonso
authors.forename: C
authors.initials: C
authors.lastname: Navarro-Ranninger
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis; D002461:Cell Line, Transformed; D002522:Chlorocebus aethiops; D002945:Cisplatin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D011905:Genes, ras; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014709:Vero Cells
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C122085:dichloro(butylamine)(isopropylamine)platinum(II); C122083:dichloro(isopropylamine)(dimethylamine)platinum(II); D002945:Cisplatin