Design and synthesis of lignostilbene-alpha,beta-dioxygenase inhibitors |
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Authors: | Han Sun young Inoue Hiroki Terada Tamami Kamoda Shigehiro Saburi Yoshimasa Sekimata Katsuhiko Saito Tamio Kobayashi Masatomo Shinozaki Kazuo Yoshida Shigeo Asami Tadao |
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Institution: | RIKEN, Hirosawa 2-1, Wako, 351-0198, Saitama, Japan. |
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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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