摘要:
Mono- and bis(platinum) complexes containing N-alkyl-ethylenediamine units of the type {cis-PtCl2[H2NCH2CH2NH(CH2)nCH(3)]} (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 H-1, C-13, 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. (C) 1999 Elsevier Science S.A. All rights reserved.