| Abstract
| - [Ru(cyclam)(bqdi)]·ZnCl4 (1·ZnCl4; cyclam = 1,4,8,11-tetraazacyclotetradecane, bqdi = o-benzoquinonediimine), [Ru(cyclam)(nqdi)]·(ClO4)2 (2·(ClO4)2; nqdi = 2,3-naphthoquinonediimine), and [Ru(cyclam)(phi)]·(ClO4)2 (3·(ClO4)2; phi = 9,10-phenanthroquinonediimine) have been prepared and evaluated for affinity to DNA and biological effects on human cancer cells.
- The synthesis and characterization of ruthenium(II) complexes, [Ru(cyclam)(bqdi)]·ZnCl4 (1·ZnCl4; cyclam = 1,4,8,11-tetraazacyclotetradecane, bqdi = o-benzoquinonediimine), [Ru(cyclam)(nqdi)]·(ClO4)2 (2·(ClO4)2; nqdi = 2,3-naphthoquinonediimine), and [Ru(cyclam)(phi)]·(ClO4)2 (3·(ClO4)2; phi = 9,10-phenanthroquinonediimine), aredescribed. The DNA binding properties and biological activity of the Ru(II) complexes were studied by variousbiophysical and cytological techniques. As expected, only 3 showed significant binding with DNA. The thermodynamicprofile of the binding of 3 and DNA was constructed by analyzing the experimental data of absorption titration andUV melting studies with the McGhee equation, van't Hoff's equation, and the Gibbs−Helmholtz equation. Compound3 binds double-stranded DNA with a binding constant of 5.0 × 104 M-1 at 20 °C, and the binding mode of thecomplex to DNA was proved to be intercalative. Cytotoxicity and induced type of cell death of 1−3 were alsoinvestigated. Basically, metal complexes with ligands of molecular shape closely related to the structure of DNAare more likely to bind DNA and possess higher toxicity.
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