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Design and synthesis of lignostilbene-alpha,beta-dioxygenase inhibitors
Authors:Han Sun young  Inoue Hiroki  Terada Tamami  Kamoda Shigehiro  Saburi Yoshimasa  Sekimata Katsuhiko  Saito Tamio  Kobayashi Masatomo  Shinozaki Kazuo  Yoshida Shigeo  Asami Tadao
Institution:RIKEN, Hirosawa 2-1, Wako, 351-0198, Saitama, Japan.
Abstract:Lignostilbene-alpha,beta-dioxygenase cleaves the olefinic double bond of phenolic stilbenes by a mechanism similar to that of 9-cis-epoxycarotenoid dioxygenase, a key enzyme in abscisic acid biosynthesis. Several analogues of stilbene were designed and synthesized, and their efficacy as inhibitors of lignostilbene-alpha,beta-dioxygenase was examined. The compound (Z)-1-(4-hydroxyphenyl)-1-fluoro-2-phenylethene (2) was found to be a potent inhibitor of this enzyme with an IC(50) of 3 microM.
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