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Synthesis of Polyamines from Ethylenediamine and Their Platinum( II ) Complexes, Potential Antitumor Agents
Author(s) -
Couri Mara Rubia Costa,
de Almeida Mauro Vieira,
Fontes Ana Paula Soares,
D’Arc Souza Chaves Joana,
Cesar Eloi Teixeira,
Alves Ricardo José,
PereiraMaia Elene Cristina,
GarnierSuillerot Arlette
Publication year - 2006
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.200501024
Subject(s) - chemistry , ethylenediamine , platinum , carboplatin , cisplatin , amine gas treating , stereochemistry , intracellular , cytotoxicity , dna , adduct , combinatorial chemistry , biochemistry , organic chemistry , in vitro , catalysis , medicine , surgery , chemotherapy
This work describes the synthesis and characterization of five new amine ligands and also the preparation and characterization of their respective platinum( II ) complexes by reaction with K 2 PtCl 4 in water. These ligands were obtained by treatment of different halides or epoxides with ethylenediamine. Cytotoxic activity and cellular accumulation of three complexes were investigated in a human small‐cell lung carcinoma cell line and its cisplatin resistant subline. The introduction of a spacer (cycle) between the two platinum atoms leads to a significant decrease in cytotoxic activity. At equitoxic doses, the intracellular platinum concentrations found for compounds 12 and 15 were significantly higher than those found for the reference compounds, cisplatin, carboplatin, or compound 9 . This fact suggests that the formation of adducts between compounds 12 and 15 and the putative pharmacological target, DNA, is less favored. If these compounds bind more slowly to DNA, interaction with other intracellular ligands such as sulfur‐containing molecules will become relevant and it may be the reason for the elevated intracellular platinum concentrations. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006)