吡啶酮核苷类似物作为DNA聚合酶底物或抑制剂的合成

Daiva Tauraitė, Rytis Ražanas, Algirdas Mikalkėnas, S. Serva, R. Meškys
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引用次数: 9

摘要

摘要:本文描述了新型无环和环吡啶酮核苷和核苷酸的合成和表征。共合成了7个核苷和4个核苷酸。所有检测的核苷均未显示出对Klenow外显子聚合酶、M.MuLV和HIV-1逆转录酶的抑制作用。以4-氯和4-溴-2-吡啶酮为核碱基的核苷酸被Klenow片段接受,但以牺牲保真度和延伸效率为代价。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of Pyridone-based Nucleoside Analogues as Substrates or Inhibitors of DNA Polymerases
ABSTRACT The synthesis and characterization of novel acyclic and cyclic pyridone-based nucleosides and nucleotides is described. In total, seven nucleosides and four nucleotides were synthesized. None of the tested nucleosides showed inhibitory properties against Klenow exo- polymerase and M.MuLV and HIV-1 reverse transcriptases. The nucleotides containing 4-chloro- and 4-bromo-2-pyridone as a nucleobase were accepted by the Klenow fragment, but at the expense of fidelity and extension efficiency.
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