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

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

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.

OriginalsprogEngelsk
TidsskriftACS Combinatorial Science
Vol/bind19
Udgave nummer10
Sider (fra-til)657-669
Antal sider13
ISSN2156-8952
DOI
StatusUdgivet - okt. 2017

ID: 185035650