期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 3, 页码 733-736出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.087
关键词
Methyltransferase inhibitor; Protein methylation; Epigenetics; Epidithiodiketopiperazines; Chaetocin
资金
- Scientific Research (C) from the Ministry of Education, Culture, Sports, Science and Technology
- RIKEN
- Grants-in-Aid for Scientific Research [24550128, 22590034] Funding Source: KAKEN
Chaetocin (1), a structurally complex epidithiodiketopiperazine (ETP) alkaloid produced by Chaetomium minutum, is a potent inhibitor of protein lysine methyltransferase G9a, which plays important roles in many biological processes. Here we present our synthetic investigations to identify a simple prototype G9a inhibitor structure based on structure-activity relationship (SAR) studies on chaetocin derivatives. The simple derivative PS-ETP-1 (14) was found to be a potent G9a inhibitor with greatly reduced cytotoxicity. (c) 2012 Elsevier Ltd. All rights reserved.
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