Identification of novel SIRT2-selective inhibitors using a click chemistry approach
Bioorganic & medicinal chemistry letters, 2014•Elsevier
A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting
two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in
the presence of Cu (I) catalyst. Screening identified two SIRT2-selective inhibitors, which
were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be
useful for further development of SIRT2-selective inhibitors.
two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in
the presence of Cu (I) catalyst. Screening identified two SIRT2-selective inhibitors, which
were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be
useful for further development of SIRT2-selective inhibitors.
Abstract
A series of 114 SIRT inhibitor candidates was assembled using ‘click chemistry’, by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors.
Elsevier