Arene Ruthenium (â…¡) Complexes Containing5-fluorouracil Derivatives: Synthesis And The Interaction With DNA

The arene ruthenium (â…¡) complexes with "half-sandwich" structureare a kind of metal anticancer drugs with high activity and low toxicitydriving much current research interests. As an anticancer drug used inclinical,5-FU had limited application since it was developed due to itslow selectivity and toxic side effect. In this paper, four prodrugs of5-FUligands were designed and synthesized by joining pyridine ring into theposition N1of5-FU using the coupling principles of drug design. IR andNMR were used to characterize their structure.Eight arene ruthenium (â…¡) complexes were synthesized by thereaction of arene-ruthenium precursors and prodrugs of5-FU ligandsusing the law of coordination. IR and NMR were used to characterizetheir structure and the DSC-TGA was used to analyze their thermalstability.The interaction of two ligands of prodrug of5-FU with CT-DNAwere researched by cyclic voltammetry. As a result, we could draw a conclude that the toxic side effect of5-FU was decreased and thecoordination ability was increased after being modified. At the same time,the interaction of eight arene ruthenium (â…¡) complexes with CT-DNAwere researched by UV-visible spectroscopy and cyclic voltammetry.The results showed that the interaction of complexes with CT-DNA wasstronger than that of its corresponding ligands. Meanwhile, theinteraction of them were not a single effect but the combination ofmultiple action. These studies would enrich the theoretical contents ofmetal anticancer drug with different active centers and provide an usefulguiding for designing new novel anticancer arene ruthenium (â…¡)complexes.