Syntheses of Ruthenium(II) Quinonediimine Complexes of Cyclam and Characterization of Their DNA-Binding Activities and Cytotoxicity

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• 作者：Hing-Leung Chan ; Heng-Qian Liu ; Biing-Chiau Tzeng ; Yuan-Shyane You ; Shie-Ming Peng ; Mengsu Yang ; and Chi-Ming Che
• 刊名：Inorganic Chemistry
• 出版年：2002
• 出版时间：June 17, 2002
• 年：2002
• 卷：41
• 期：12
• 页码：3161 - 3171
• 全文大小：280K
• 年卷期：v.41,no.12(June 17, 2002)
• ISSN：1520-510X

文摘

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.