Ontology highlight
ABSTRACT:
SUBMITTER: Vaidya AS
PROVIDER: S-EPMC3401313 | biostudies-literature | 2012 Aug
REPOSITORIES: biostudies-literature
Vaidya Aditya Sudheer AS Karumudi Bhargava B Mendonca Emma E Madriaga Antonett A Abdelkarim Hazem H van Breemen Richard B RB Petukhov Pavel A PA
Bioorganic & medicinal chemistry letters 20120618 15
The design, modeling, synthesis, biological evaluation of a novel series of photoreactive benzamide probes for class I HDAC isoforms is reported. The probes are potent and selective for HDAC1 and 2 and are efficient in crosslinking to HDAC2 as demonstrated by photolabeling experiments. The probes exhibit a time-dependent inhibition of class I HDACs. The inhibitory activities of the probes were influenced by the positioning of the aryl and alkyl azido groups necessary for photocrosslinking and at ...[more]