Identification of novel SIRT2-selective inhibitors using a click chemistry approach

Identification of novel SIRT2-selective inhibitors using a click chemistry approach
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DOI：
10.1016/j.bmcl.2014.03.026
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发表时间：
2014-04-15
期刊：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
影响因子：
2.7
通讯作者：
Suzuki, Takayoshi
Suzuki, Takayoshi
中科院分区：
医学4区
文献类型：
--
作者：
Tatum, Prima R.;Sawada, Hideyuki;Suzuki, Takayoshi

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使用“点击化学”，通过在Cu（I）催化剂存在下使两个带有2-苯胺基苯甲酰胺药效团的炔与57个叠氮化物结构单元反应，组装了一系列114种SIRT抑制剂候选物。筛选鉴定了两种SIRT 2选择性抑制剂，其比已知的SIRT 2抑制剂AGK 2更具SIRT 2选择性。这些发现将有助于SIRT 2选择性抑制剂的进一步开发。(C)2014爱思唯尔有限公司版权所有。
A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu( I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.