title: Synthesis, characterization, cytotoxic activity, and cellular accumulation of dinuclear platinum complexes derived from N,N'-di-(2-aminoethyl)-1,3-diamino-2-propanol, aryl substituted N-benzyl-1,4-butanediamines, and N-benzyl-1,6-hexanediamines.
abstract: This work describes the synthesis and characterization of six new dinuclear platinum complexes having N,N'-di-(2-aminoethyl)-1,3-diamino-2-propanol, aryl substituted N-benzyl-1,4-butanediamines and N-benzyl-1,6-hexanediamines as ligands. They were prepared by the reaction of cis-[PtCl(2)(DMSO)(2)] (DMSO=dimethyl sulfoxide) with the appropriate ligand in water, except for one of them, which was prepared from K(2)PtCl(4). We also report the cytotoxic activity and cellular accumulation of three of these complexes in a human small-cell lung carcinoma cell line and its resistant subline. Resistant cells exhibited a lesser degree of cross-resistance to these compounds when compared to cisplatin. The accumulation of platinum in both cell lines followed the same pattern, i.e. approximately the same intracellular platinum concentration yielded the same cytotoxic effect independent of the nature of the platinum complex used.
authors.affiliation: Colégio de Aplicação João XXIII, Juiz de Fora-MG, Brazil.
authors.forename: Elói Teixeira
authors.initials: ET
authors.lastname: Cesar
authors.forename: Mauro Vieira
authors.initials: MV
authors.lastname: de Almeida
authors.forename: Ana Paula Soares
authors.initials: AP
authors.lastname: Fontes
authors.forename: Elene Cristina
authors.initials: EC
authors.lastname: Pereira Maia
authors.forename: Arlette
authors.initials: A
authors.lastname: Garnier-Suillerot
authors.forename: Mara
authors.initials: M
authors.lastname: Rúbia Costa Couri
authors.forename: Emanoel
authors.initials: E
authors.lastname: de Castro Antunes Felício
mesh_terms: D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D019008:Drug Resistance, Neoplasm; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity*; D010984:Platinum / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity*; D011700:Putrescine / Q000031:analogs & derivatives* / Q000737:chemistry*
chemical_list: D008024:Ligands; D009944:Organoplatinum Compounds; C061106:N-benzylputrescine; D010984:Platinum; D011700:Putrescine