Macrocyclic Peptoid–Peptide Hybrids as Inhibitors of Class I Histone Deacetylases

Christian Adam Olsen, Ana Montero, Luke J. Leman, M. Reza Ghadiri

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

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 cell lines.
Original languageEnglish
JournalA C S Medicinal Chemistry Letters
Volume3
Pages (from-to)749-753
ISSN1948-5875
Publication statusPublished - 2012

Keywords

  • HDAC inhibitors
  • Peptides
  • Peptoids
  • Macrocycles
  • Apicidin

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