Combined Chemical and Biosynthetic Route to Access a New Apoptolidin Congener

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• 作者：Victor P. Ghidu ; Ioanna Ntai ; Jingqi Wang ; Aaron T. Jacobs ; Lawrence J. Marnett ; Brian O. Bachmann ; Gary A. Sulikowski
• 刊名：Organic Letters
• 出版年：2009
• 出版时间：July 16, 2009
• 年：2009
• 卷：11
• 期：14
• 页码：3032-3034
• 全文大小：156K
• 年卷期：v.11,no.14(July 16, 2009)
• ISSN：1523-7052

文摘

Glycosylation of a synthetic aglycone using precursor-directed biosynthesis is facilitated by a chemical ketosynthase “knockdown” of the apoptolidin producer Nocardiopsis sp. This synthetic approach facilitated the preparation of an unnatural disaccharide derivative of apoptolidin D that substantially restores cytotoxicity against H292 cells and deconvolutes the role of the decorating sugars in apoptolidin bioactivity.