Reengineering an Azaphilone Biosynthesis Pathway in Aspergillus nidulans To Create Lipoxygenase Inhibitors

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Title:	Reengineering an Azaphilone Biosynthesis Pathway in Aspergillus nidulans To Create Lipoxygenase Inhibitors
Authors:	Somoza, Amber D. Lee, Kuan-Han Chiang, Yi-Ming Oakley, Berl R. Wang, Clay C.C.
Contributors:	藥學系
Keywords:	Oxidative Dearomatization Catalysis Product Acid
Date:	2012-02-17
Issue Date:	2014-03-21 16:17:35 (UTC+8)
Publisher:	Amer Chemical Soc
Abstract:	Sclerotiorin, an azaphilone polyketide, is a bioactive natural product known to inhibit 15-lipoxygenase and many other biological targets. To readily access sclerotiorin and analogs, we developed a 2-3 step semisynthetic route to produce a variety of azaphilones starting from an advanced, putative azaphilone intermediate (5) overproduced by an engineered strain of Aspergillus nidulans. The inhibitory activities of the semisynthetic azaphilones against 15-lipoxygenase were evaluated with several compounds displaying low micromolar potency.
Relation:	Organic Letters, 14(4), 972-975
Appears in Collections:	[Dept. of Pharmacy] Periodical Articles

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