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 language | English |
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Journal | A C S Combinatorial Science |
Volume | 19 |
Issue number | 10 |
Pages (from-to) | 657-669 |
ISSN | 2156-8952 |
DOIs | |
Publication status | Published - 2017 |
Keywords
- HDAC inhibitor
- Hydroxamic acid
- Linker
- Solid-phase synthesis