Synthesis of NF-κB activation inhibitors derived from epoxyquinomicin C

N Matsumoto, A Ariga, S To-e, H Nakamura…

Index: Matsumoto, Naoki; Ariga, Akiko; To-E, Sakino; Nakamura, Hikaru; Agata, Naoki; Hirano, Shin-Ichi; Inoue, Jun-Ichiro; Umezawa, Kazuo Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 9 p. 865 - 869

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Citation Number: 150

Abstract

In order to develop new inhibitors of NF-κB activation, we designed and synthesized dehydroxymethyl derivatives of epoxyquinomicin C, namely, DHM2EQ and its regioisomer DHM3EQ. These derivatives were synthesized from 2, 5-dimethoxyaniline in 5 steps. Since DHM2EQ was more active and less toxic than DHM3EQ, its stereochemical configuration was determined by X-ray crystallographic analysis. Each enantiomer of the protected ...