【摘要】 本文以自组装法制得的双链DNA(ds-DNA)和G-四链体DNA(G4-DNA)修饰的金电极为工作电极,以Fe(CN)63-/4-为电活性指示剂,采用循环伏安法和微分脉冲伏安法研究了非电活性苯磺酰类5-氟尿嘧啶衍生物与ds-DNA和G4-DNA的相互作用.实验结果表明:苯磺酰类5-氟尿嘧啶与ds-DNA或G4-DNA的结合常数与苯环上邻、对位取代基的得失电子能力密切相关,强吸电子基团取代有利于苯磺酰类5-氟尿嘧啶选择性结合G-四链体DNA.更多还原

【Abstract】 The interaction of double-stranded (ds) and G-quadruplex (G4) DNA with sulfonyl 5-fluorouracil derivatives (5-fluoro-1-(arylsulfonyl) pyrimidine-2,4(1H,3H)-diones) was investigated in this research, in which Au electrodes modified with ds-DNA or G4-DNAs were used as a working electrode. The investigation showed that the binding affinity with G4-DNA was significantly increased when 5-fluorouracil (5-FU) was modified with arylsulfonyl groups. The presence of strong electron-withdrawing groups on benzene sulfonyl 5-FU greatly enhanced the binding selectivity (kG4-DNA/kds-DNA). Such results provided new insights into the potential connections between the chemical structure of drug candidates and their anticancer activities.更多还原