Abstract：
The role of G-quadruplex (G4) in cellular processes can be investigated by the covalent modification of G4-DNA using alkylating reagents. Controllable alkylating reagents activated by external stimuli can react elegantly and selectively. Herein, we report a chemical activation system that can significantly boost the reaction rate of methylamine-protected vinyl-quinazolinone (VQ) derivative for the alkylation of G4-DNA. The two screened activators can transform low-reactive VQ-NHR\' to highly reactive intermediates following the Michael addition mechanism. This approach expands the toolbox of activable G4 alkylating reagents.
摘要：
G-四链体（G4）在细胞过程中的作用可以通过使用烷基化试剂对G4-DNA进行共价修饰来研究。由外部刺激激活的可控烷基化试剂可以优雅而选择性地反应。在这里，我们报道了一种化学活化系统，该系统可以显着提高甲胺保护的乙烯基喹唑啉酮（VQ）衍生物用于G4-DNA烷基化的反应速率。两种筛选的活化剂可以按照迈克尔加成机理将低反应性VQ-NHR转化为高反应性中间体。该方法扩展了可活化的G4烷基化试剂的工具箱。
