期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 21, 页码 5260-5262出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.09.048
关键词
PROTACs; Thalidomide; Cereblon; E3 ligase
资金
- Helmholtz Drug Research Initiative (Helmholtz Wirkstoffforschung)
The use of small molecules to regulate cellular levels of specific proteins is poised to become a powerful technique in the coming years. Critical to the success of any project utilizing such an approach will be the ability to synthesize libraries of candidate small molecules for testing in cellular systems. Herein, we describe a practical synthesis of a phthalimide-based scaffold, which can be easily diversified to make Cereblon-targeting PROTACs. We demonstrate the effectiveness of this approach by synthesizing a 'PROTAC toolbox' of four amines which can be coupled to inhibitors in a straightforward manner. (C) 2016 Elsevier Ltd. All rights reserved.
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