487003-96-3Relevant academic research and scientific papers
A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
Bang, Claus G.,Jensen, Jakob F.,O'Hanlon Cohrt, Emil,Olsen, Lasse B.,Siyum, Saba G.,Mortensen, Kim T.,Skovgaard, Tine,Berthelsen, Jens,Yang, Liang,Givskov, Michael,Qvortrup, Katrine,Nielsen, Thomas E.
, p. 657 - 669 (2017)
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.
