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A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2017-09-06 00:00:00 , DOI: 10.1021/acscombsci.7b00068
Claus G. Bang 1 , Jakob F. Jensen 1 , Emil O’Hanlon Cohrt 1 , Lasse B. Olsen 1 , Saba G. Siyum 1 , Kim T. Mortensen 1 , Tine Skovgaard 2 , Jens Berthelsen 2 , Liang Yang 3 , Michael Givskov 2, 3 , Katrine Qvortrup 1 , Thomas E. Nielsen 1, 2, 3
Affiliation  

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.

中文翻译:

固相合成异羟肟酸和鉴定HDAC6抑制剂的连接物

我们在此提出了广泛有用的,容易获得的和非整体的羟胺连接基,用于羟肟酸的常规固相合成。所开发的方案能够有效地合成和释放各种树脂中的各种异羟肟酸,这取决于试剂和合成方法的高度控制和灵活性。基于三苯甲基的羟胺接头用于合成肽异羟肟酸的文库。使用基于化学发光的测定法检查了化合物对7种HDAC酶亚型的抑制作用。
更新日期:2017-09-06
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