Ontology highlight
ABSTRACT:
SUBMITTER: Canzoneri JC
PROVIDER: S-EPMC2783919 | biostudies-literature | 2009 Dec
REPOSITORIES: biostudies-literature
Canzoneri Joshua C JC Chen Po C PC Oyelere Adegboyega K AK
Bioorganic & medicinal chemistry letters 20091013 23
We describe herein the synthesis and characterization of a new class of histone deacetylase (HDAC) inhibitors derived from conjugation of a suberoylanilide hydroxamic acid-like aliphatic-hydroxamate pharmacophore to a nuclear localization signal peptide. We found that these conjugates inhibited the histone deacetylase activities of HDACs 1, 2, 6, and 8 in a manner similar to suberoylanilide hydroxamic acid (SAHA). Notably, compound 7b showed a threefold improvement in HDAC 1/2 inhibition, a thre ...[more]