{Reference Type}: Journal Article
{Title}: Michael addition-activated alkylation of G-quadruplex DNA with methylamine-protected vinyl-quinazolinone derivatives.
{Author}: Chen Y;Onizuka K;Nagatsugi F;
{Journal}: Bioorg Med Chem Lett
{Volume}: 109
{Issue}: 0
{Year}: 2024 Sep 1
{Factor}: 2.94
{DOI}: 10.1016/j.bmcl.2024.129855
{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.