1202186-19-3Relevant academic research and scientific papers
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide
Canzoneri, Joshua C.,Chen, Po C.,Oyelere, Adegboyega K.
supporting information; experimental part, p. 6588 - 6590 (2010/06/12)
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 threefold increase in HDAC 6 selectivity and a twofold increase in HDAC 8 selectivity when compared to SAHA.
