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

Research output: Contribution to journalJournal articleResearchpeer-review

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
JournalACS Combinatorial Science
Issue number10
Pages (from-to)657-669
Number of pages13
Publication statusPublished - Oct 2017

    Research areas

  • HDAC inhibitor, hydroxamic acid, linker, solid-phase synthesis

ID: 185035650