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. 2002 Apr 22;12(8):1139-42.
doi: 10.1016/s0960-894x(02)00126-9.

Design and synthesis of lignostilbene-alpha,beta-dioxygenase inhibitors

Sun young Han  1 , Hiroki Inoue, Tamami Terada, Shigehiro Kamoda, Yoshimasa Saburi, Katsuhiko Sekimata, Tamio Saito, Masatomo Kobayashi, Kazuo Shinozaki, Shigeo Yoshida, Tadao Asami
Affiliations

Design and synthesis of lignostilbene-alpha,beta-dioxygenase inhibitors

Sun young Han et al. Bioorg Med Chem Lett. .

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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