1 research outputs found
Multiply Intercalator-Substituted Cu(II) Cyclen Complexes as DNA Condensers and DNA/RNA Synthesis Inhibitors
Many drugs that are
applied in anticancer therapy such as the anthracycline doxorubicin
contain DNA-intercalating 9,10-anthraquinone (AQ) moieties. When CuÂ(II)
cyclen complexes were functionalized with up to three (2-anthraquinonyl)Âmethyl
substituents, they efficiently inhibited DNA and RNA synthesis resulting
in high cytotoxicity (selective for cancer cells) accompanied by DNA
condensation/aggregation phenomena. Molecular modeling suggests an
unusual bisintercalation mode with only one base pair between the
two AQ moieties and the metal complex as a linker. A regioisomer,
in which the AQ moieties point in directions unfavorable for such
an interaction, had a much weaker biological activity. The ligands
alone and corresponding ZnÂ(II) complexes (used as redox inert control
compounds) also exhibited lower activity