Synthesis and biological activity of cis-dichloro mono- and bis(platinum) complexes with N-alkyl-ethylenediamine ligands |
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Authors: | Bernhard Miller Stefan Wild Haralabos Zorbas Wolfgang Beck |
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Institution: | a Institut für Anorganische Chemie der Universität München, Butenandstraße 5-13, D-81377 Munich, Germany b Institut für Biochemie der Universität München, Feodor-Lynen-Straße 25, D-81377 Munich, Germany |
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Abstract: | Mono- and bis(platinum) complexes containing N-alkyl-ethylenediamine units of the type {cis-PtCl2H2NCH2CH2NH(CH2)nCH3]} (n=8, 9, 11, 15) and {cis-PtCl2(H2NCH2CH2NH)}2(CH2)n] (n=6, 8, 10, 12) and their corresponding dihydroxo-platinum(IV) complexes were synthesized. The structures of the metal chelates were derived from elemental analyses and their 1H, 13C, IR spectra. The length of the aliphatic chains has been varied systematically, in order to increase the lipophilicity. Enlargement of the linker could also lead to more flexibility of one platinum sphere in reference to the attached DNA species. Using in vitro cytotoxicity tests it is shown that the biological activity of the bis(platinum) complexes increased, up to n=12, with the length of the linker. The longest linker in the ligands resulted in the most effective bis(platinum) complexes against L1210 murine leukemia cells. |
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Keywords: | Biological activity Platinum complexes Ethylenediamine complexes |
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