Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases.
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ABSTRACT:
SUBMITTER: Olsen CA
PROVIDER: S-EPMC4025818 | biostudies-other | 2012 Sep
REPOSITORIES: biostudies-other
Publications
Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases.
Olsen Christian A CA Montero Ana A Leman Luke J LJ Ghadiri M Reza MR
ACS medicinal chemistry letters 20120810 9
We report the design, synthesis, and biological evaluation of the first macrocyclic peptoid-containing histone deacetylase (HDAC) inhibitors. The compounds selectively inhibit human class I HDAC isoforms in vitro, with no inhibition of the tubulin deacetylase activity associated with class IIb HDAC6 in cultured Jurkat cells. Compared to the natural product apicidin (1), one inhibitor (compound 10) showed equivalent potency against K-562 cells, but was more cytoselective across a panel of cancer ...[more]
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