Reengineering an azaphilone biosynthesis pathway in Aspergillus nidulans to create lipoxygenase inhibitors.

Reengineering an azaphilone biosynthesis pathway in Aspergillus nidulans to create lipoxygenase inhibitors.
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DOI:
10.1021/ol203094k
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发表时间:
2012-02-17
期刊:
影响因子:
5.2
通讯作者:
Wang CC
Wang CC
中科院分区:
化学1区
文献类型:
--
作者:
Somoza AD;Lee KH;Chiang YM;Oakley BR;Wang CC

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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) over-produced 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.
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