Journal article
A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
Department of Chemistry1
The Costerton Biofilm Center, Department of Immunology and Microbiology2
Singapore Centre for Environmental Life Sciences Engineering3
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.
Language: | English |
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Publisher: | American Chemical Society |
Year: | 2017 |
Pages: | 657-669 |
ISSN: | 21568944 and 21568952 |
Types: | Journal article |
DOI: | 10.1021/acscombsci.7b00068 |