Described herein are 5-position modified cytosines of formula I, nucleotides and nucleosides as well as phosphoramidites and triphosphates derivatives thereof. Further provided are methods of making and using the same, and compositions and uses of the modified nucleosides as part of a nucleic acid molecule (e.g., aptamer). Those modified nucleotides, bearing an N-substituted-carboxamine group at the 5 -position, are valuable tools for improving in vitro selection of protein-binding aptamers (SELEX process).
wherein
R is independently a -(CH2)n, wherein n is 0,1,2,3,4,5,6,7,8,9 or 10;
RX1 is independently selected from the group consisting of
本文描述了式 I 的 5 位修饰
胞嘧啶、核苷酸和核苷及其
磷酰胺和
三磷酸酯衍
生物。此外,还提供了制造和使用这些核苷酸的方法,以及作为核酸分子(如适
配体)一部分的修饰核苷酸的组合物和用途。这些在 5-位上带有 N-取代-甲酰胺基团的修饰核苷酸是改进体外选择蛋白质结合适
配体(
SELEX 过程)的重要工具。
其中
R 独立地为-(
CH2)n,其中 n 为 0、1、2、3、4、5、6、7、8、9 或 10;
RX1 独立地选自以下组成的组