DNA targeted platinum complexes: Synthesis, cytotoxicity and DNA interactions of cis-dichloroplatinum(II) complexes tethered to phenazine-1- carboxamides

Leah C. Perrin, Paul D. Prenzler, Carleen Cullinane, Don R. Phillips, William A. Denny, W. David McFadyen

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)

Abstract

A series of intercalator-tethered platinum(II) complexes PtLCl2 have been prepared, where L are the diamine ligands N-[2- [(aminoethyl)amino]ethyl]-phenazine-1-carboxamide, N-[3-[(2- aminoethyl)amino]propyl]-phenazine-1-carboxamide, N-[4-[(2- aminoethyl)amino]butyl]-phenazine-1-carboxamide and N-[5- [(aminoethyl)amino]pentyl]-phenazine-1-carboxamide. Measurements of the time- course of unwinding of supercoiled pUC19 plasmid DNA by the phenazine complexes PtLCl2 reveal that the presence of the intercalator leads to enhanced rates of DNA platination when compared with the complex Pt(en)Cl2. The platinum(II) complexes where the polymethylene linker chain contains three, four or five carbon atoms are considerably more cytotoxic against murine P388/W than either cisplatin, Pt(en)Cl2, or the metal-free ligands themselves. (C) 2000 Elsevier Science S.A.

Original languageEnglish
Pages (from-to)111-117
Number of pages7
JournalJournal of Inorganic Biochemistry
Volume81
Issue number1-2
DOIs
Publication statusPublished - 15 Jul 2000

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