The DNA/Triplex RNA-Binding And Topos Inhibition Of Ruthenium(Ⅱ) Complexes

After entering a brand new century, along with the science technology andeconomy develops in a fast pace，every academic discipline also has great changes.Among this, driven by the growing of life sciences and the actual needs of medicine,environment, Bioinorganic Chemistry is in a great explosion, becoming a maturesubject. Between the studies on Bioinorganic Chemistry not only at home，but also atabroad, the studies on the structures and properties of metal/nonmetal binding withnucleic acid are the most important area. Additionally, ruthenium complexes get a lotof attractions for their own advantages. Therefore, many ruthenium complexes of newstructures are synthesized and used for more studies.This thesis can be mainly described as the following chapters：Chapter1. The basic knowledge of nucleic acid, such as DNA, RNA, and DNAtopoisomerases were presented. Then the DNA binding and topoisomerases inhibitionof ruthenium(II) complexes were also briefly introduced．Chapter2. Two Ru(II) complexes [Ru(bpy)2(mip)]2+(Ru1) and[Ru(bpy)2(bdip)]2+(Ru2) which contain the same ancillary ligand and different mainligands were synthesized. We used1H NMR, mass spectra and elemental analyses tocharacterize the synthesized complexes. U·A*U binding properties of these two Ru (II)complexes had been investigated via UV-vis spectral titration, fluorescence spectra,U·A*U-thermal denaturation, and CD spectra. Moreover, density-function-theory-based quantum chemistry calculations had been used to explain theU·A*U-binding properties of the synthesized Ru (II) complexes and the stabilizationof the third chain. The results show that both complexes have function on thestabilization of the third chain, especially Ru1binds much more strong.Chapter3. We had designed and synthesized another two Ru(II) complexesRu(bpy)2L(Ru3) and Ru(phen)2L(Ru4), contained the same intercalative-ligand butdifferent ancillary-ligands. By means of1H NMR, MS and elemental analyses, thesetwo complexes had already been well characterized. Then the bind characteristics ofDNA and Ru (II) complexes could be well explained after several tests. Furthermore,gel-electrophoresis had been used to explore the photo cleavage of the DNA by theRu(II) complexes and its mechanism．The result of all these experiments show that:these two complexes bind to DNA by an intercalative mode, and they are effectivephoto cleavage agents. Chapter4. In this part, we had studied and discussed the DNA topoisomerasesinhibition of two complexes in Chapter3via gel-electrophoresis measurement. Theexperiments show that both of these two Ru (II) complexes are proved to be dualTopo I/II inhibitors.