Portal de Periódicos da CAPES

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

2017; American Chemical Society; Volume: 19; Issue: 10 Linguagem: Inglês

10.1021/acscombsci.7b00068

2156-8952

Claus G. Bang, Jakob F. Jensen, Emil O’Hanlon Cohrt, Lasse B. Olsen, Saba G. Siyum, Kim T. Mortensen, Tine Skovgaard, Jens Berthelsen, Liang Yang, Michael Givskov, Katrine Qvortrup, Thomas E. Nielsen,

Chemical Synthesis and Analysis

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.