Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase

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题名:	Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase
作者:	Lin, Y.-L., Huang, J.-L., Wu, C.-S., Liu, H.-G., Yang, D.-Y.
贡献者:	Department of Chemistry, Tunghai University
日期:	2002
上传时间:	2013-05-14T09:03:54Z (UTC)
摘要:	An epoxybenzoquinone, 4-hydroxyphenoxypropionic acid, and 2-hydroxy-3-phenyl-3-butenoic acid derivatives have been designed, synthesized, and evaluated for in vitro inhibition activity against 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) from pig liver by the spectrophotometric enol-borate method. The biological data demonstrated that neither epoxybenzoquinone ester nor 2-hydroxy-3-phenyl-3-butenoic acid is an inhibitor of 4-HPPD. The most potent 4-HPPD inhibitor tested was 3-hydroxy-4-phenyl-2(5H)-furanone with an IC 50 value of 0.5 μM, which may serve as a lead compound for further design of more potent 4-HPPD inhibitors. ? 2002 Elsevier Science Ltd. All rights reserved.
關聯:	Bioorganic and Medicinal Chemistry Letters Volume 12, Issue 13, 8 July 2002, Pages 1709-1713
显示于类别:	[化學系所] 期刊論文

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