Synthesis, GC selective DNA binding and topoisomerase II inhibition activities of ruthenium(II) polypyridyl complex containing 11-aminopteridino[6,7-f][1,10]phenanthrolin-13(12H)-one.

Feng Gao, Hui Chao, Feng Zhou, Xin Chen, Yuan-Fang Wei, Liang-Nian Ji

MOE Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, PR China.

Journal of inorganic biochemistry 2008 May-Jun

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A DNA-intercalating Ru(II) polypyridyl complex [Ru(bpy)2(appo)]2+ (bpy=2,2'-bipyridine, appo=11-aminopteridino[6,7-f][1,10]phenanthrolin-13(12H)-one) has been synthesized and characterized by elemental analysis, electrospray mass spectra, (1)H NMR, UV/Vis spectrum, fluorescent spectrum and electrochemistry. The DNA-binding, photocleavage, and topoisomerase inhibition of the complex was studied. Interestingly, the complex binds to DNA via an intercalative mode with preference for GC sequences and cleaves the pBR322 DNA upon irradiation. In addition, the complex shows high inhibition activity against topoisomerase II by interfere the DNA religation.

Citation

Feng Gao, Hui Chao, Feng Zhou, Xin Chen, Yuan-Fang Wei, Liang-Nian Ji. Synthesis, GC selective DNA binding and topoisomerase II inhibition activities of ruthenium(II) polypyridyl complex containing 11-aminopteridino[6,7-f][1,10]phenanthrolin-13(12H)-one. Journal of inorganic biochemistry. 2008 May-Jun;102(5-6):1050-9