Journal article
A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
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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Year: | 2017 |
Pages: | 657-669 |
ISSN: | 21568944 and 21568952 |
Types: | Journal article |
DOI: | 10.1021/acscombsci.7b00068 |
ORCIDs: | 0000-0002-9225-1995 , Qvortrup, Katrine , 0000-0001-8700-1951 and 0000-0001-5004-8609 |