Document Report Card

ID: ALA1147150

Journal: J Med Chem

Title: Design and synthesis of a potent histone deacetylase inhibitor.

Authors: Liu T, Kapustin G, Etzkorn FA.

Abstract: Histone deacetylase (HDAC) inhibitors have potential for cancer therapy. An HDAC inhibitor based on a cyclic peptide mimic of known structure, linked by an aliphatic chain to a hydroxamic acid, was designed and synthesized. The chimeric compound showed potent competitive inhibition of nuclear HDACs, with an IC50 value of 46 nM and a Ki value of 13.7 nM. The designed inhibitor showed 4-fold selectivity for HDAC1 (57 nM) over HDAC8 (231 nM).

CiteXplore: 17419603

DOI: 10.1021/jm061082q