期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 8, 页码 2343-2345出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.117
关键词
Proteasome; Inhibitor; Boronic acid; Centrifugal liquid-liquid partition chromatography
Boronic acid derivatives of tyropeptin were synthesized with TP-110 as the lead compound. Due to the lability of the aminoboronic acid moiety, careful design of the deprotection and coupling sequence was required. Liquid-liquid partition chromatography was found to be a powerful tool for purification of compounds of this class. The obtained derivatives showed potent inhibitory activities against the human 20S proteasome in vitro. (C) 2009 Elsevier Ltd. All rights reserved.
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