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Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.

Bioorganic & medicinal chemistry letters (2009-10-27)
Joshua C Canzoneri, Po C Chen, Adegboyega K Oyelere
ABSTRACT

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.

MATERIALS
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Brand
Product Description

Sigma-Aldrich
O-Tritylhydroxylamine, 95%

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