Efficient synthesis of (±)-parasitenone, a novel inhibitor of NF-κB

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• 作者：Tsuyoshi Saitoh ; Eriko Suzuki ; Arisa Takasugi ; Rika Obata ; Yuichi Ishikawa ; Kazuo Umezawa ; Shigeru Nishiyama
• 关键词：NF-κ ; B inhibitor ; DHMEQ ; Parasitenone ; Anodic oxidation ; Epoxycyclohexenone
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 September 2009
• 年：2009
• 卷：19
• 期：18
• 页码：5383-5386
• 全文大小：480 K

文摘

Dehydroxymethylepoxyquinomicin (DHMEQ, 1) is a novel nuclear factor-κB (NF-κB) inhibitor that inhibits DNA binding of NF-κB components including p65. To inspect its biological activity of 1, we synthesized parasitenone (3), possessing the common epoxycyclohexenone moiety of 1. Assessment of the inhibitory activity against NF-κB indicated that the epoxycyclohexenone moiety is the most essential element for the NF-κB inhibitory activity and the salicylic acid moiety may contribute the binding efficiency and specificity.