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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.
NF-kappaB is a transcription factor that induces the expression of inflammatory cytokines and antiapoptotic proteins. Earlier we designed a new NF-kappaB inhibitor, (-)-DHMEQ, and showed that it had potent anticancer and anti-inflammatory activities in various animal models without any toxicity. In the present research, we studied whether (-)-DHMEQ could be… (More)