ChemInform Abstract: Synthesis, Characterization, and DNA-Binding Properties of (1,2-Diaminoethane)platinum(II) Complexes Linked to the DNA Intercalator Acridine Orange by Trimethylene and Hexamethylene Chains.
Abstract
Details of the preparation of the Pt complexes (VIc) and (VIe) (see scheme) as well as X-ray structure determinations of the oxalato derivative (VIII) (P1, Z=2), which forms suitable crystals, and the ligand precursors (Ia) (C2/c, Z = 8) and (Ib) (P1, Z=2) are reported.
ChemInform Abstract
Details of the preparation of the Pt complexes (VIc) and (VIe) (see scheme) as well as X-ray structure determinations of the oxalato derivative (VIII) (P1, Z=2), which forms suitable crystals, and the ligand precursors (Ia) (C2/c, Z = 8) and (Ib) (P1, Z=2) are reported. The interaction of (VIc) and (VIe) with DNA is studied by absorption spectroscopy. These results together with the previously reported covalent binding to, and superhelical unwinding of, DNA by (VIc) support a model in which the platinum moiety binds covalently to DNA while the acridine orange moiety is intercalated one or two base pairs away. The strategy employed for linking Pt to DNA-intercalating molecules suggests possibilities for preparing new compounds for studying anticancer platinum drug binding to DNA and could ultimately lead to clinically more effective antitumor drugs.
