一种基于 DHMEQ 的氨基环氧喹啉核心的新型 NF-κB 抑制剂。
A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ.
机构信息
Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5638-42. doi: 10.1016/j.bmcl.2010.08.036. Epub 2010 Aug 11.
PMID:20801656
Abstract
The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.
摘要
氨基-环氧喹啉 6a 和 6b 被合成作为 NF-κB 抑制剂 DHMEQ（1）的可溶性衍生物。尽管 6b 的构型与 1 相反，但基于 NO 分泌和 MALDI-TOF MS 分析，是 6b 而不是 6a 影响了 NF-κB 的失活。这表明 6b 通过与 1 不同的方式抑制了激活。
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