Synthesis and evaluation of a cyclopropane derivative of DHMEQ

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概要

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• DHMEQ (1) is well known to inhibit NF-κB, which is closely associated with immune, inflammatory, and apoptotic processes as an inducible transcription factor. The inhibitory effect seems to be the result of the ring opening of an epoxide of 1 with Cys38 of p65. We have synthesized an analog 4 containing a cyclopropanated quinol skeleton and examined its ability to inhibit NF-κB. Surprisingly, 4 showed no remarkable NF-κB inhibitory activity as determined through expression of COX-2 in an RAW264.7 macrophage cell line.

著者

• Nakago Takahiro

  Department of Applied Chemistry, Kogakuin University

関連論文

• Synthesis and evaluation of a cyclopropane derivative of DHMEQ

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