A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors

Claus Gunnar Bang, Jakob Feldthusen Jensen, Anders Emil O'Hanlon Cohrt, Lasse Bohn Olsen, Saba Gebremedhin Siyum, Kim Thollund Mortensen, Tine Skovgaard, Jens Berthelsen, Liang Yang, Michael Givskov, Katrine Qvortrup, Thomas Eiland Nielsen

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

We herein present broadly useful, readily available and nonintegral hydroxylamine linkers for the routine solid-phase synthesis of hydroxamic acids. The developed protocols enable the efficient synthesis and release of a wide range of hydroxamic acids from various resins, relying on high control and flexibility with respect to reagents and synthetic processes. A trityl-based hydroxylamine linker was used to synthesize a library of peptide hydroxamic acids. The inhibitory effects of the compounds were examined for seven HDAC enzyme subtypes using a chemiluminescence-based assay.
Original languageEnglish
JournalA C S Combinatorial Science
Volume19
Issue number10
Pages (from-to)657-669
ISSN2156-8952
DOIs
Publication statusPublished - 2017

Keywords

  • HDAC inhibitor
  • Hydroxamic acid
  • Linker
  • Solid-phase synthesis

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