PHOTOREACTIVE BENZAMIDE PROBES FOR HISTONE DEACETYLASE 2

摘要

The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.

主权项

1. A compound of formula (I): or a salt, hydrate or solvate thereof, wherein: X is selected from the group consisting of azido, aryl, substituted aryl, heteroaryl and substituted heteroaryl; each Y is independently selected from the group consisting of hydrogen, alkyl and substituted alkyl; R1, R2 and R3 are independently selected from the group consisting of hydrogen, azido, azidoalkyl, azidoalkoxy, and azidoalkylamidyl, wherein at least one of R1, R2 and R3 is selected from the group consisting of azido, azidoalkyl, azidoalkoxy, and azidoalkylamidyl; and rings A and B are optionally further substituted with one or more substituents selected from the group consisting of halo, alkyl, alkoxy, aryl and acyl.