An antisense oligonucleotide is expected as an innovative drug for cancer and hereditary diseases. In this paper, we designed and synthesized DNAs containing a novel nucleoside analog, 1-(4-C-aminomethyl-2-deoxy-2-fluoro-β-d-arabinofuranosyl)thymine, and evaluated their properties. It was revealed that the analog slightly decreases the thermal stability of the DNA/RNA duplex but significantly increases the stability of DNA in a buffer containing bovine serum. Furthermore, it turned out that the DNA/RNA duplex containing the analog is a good substrate for Escherichia coli RNase H. Thus, DNAs containing the nucleoside analog would be good candidates for the development of therapeutic antisense oligonucleotides.

预计反义寡核苷酸将成为治疗癌症和遗传性疾病的创新药物。在本文中，我们设计并合成了包含新型核苷类似物1-（4 - C-氨基甲基-2-脱氧-2-氟-β- d-阿拉伯呋喃糖基）胸腺嘧啶的DNA ，并评估了它们的特性。揭示了类似物稍微降低了DNA / RNA双链体的热稳定性，但是显着提高了在含有牛血清的缓冲液中DNA的稳定性。此外，事实证明，包含类似物的DNA / RNA双链体是大肠杆菌RNase H的良好底物。因此，包含核苷类似物的DNA将是开发治疗性反义寡核苷酸的良好候选者。