New Sources of Chemical Diversity Inspired by Biosynthesis: Rational Design of a Potent Epothilone Analogue

被引：13
作者：
Frein, Jeffrey D. [1 ,2 ]
Taylor, Richard E. [1 ,2 ]
Sackett, Dan L. [3 ]
机构：
[1] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA
[2] Univ Notre Dame, Walther Canc Res Ctr, Notre Dame, IN 46556 USA
[3] NICHHD, Lab Integrated & Med Biophys, NIH, Bethesda, MD 20892 USA
来源：
ORGANIC LETTERS | 2009年 / 11卷 / 15期
关键词：
CONFORMATION-ACTIVITY RELATIONSHIPS; POLYKETIDE NATURAL-PRODUCTS; CHLORIDE; REAGENTS; BINDING;
D O I：
10.1021/ol900971r
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A concise total synthesis of (S)-14-methoxyepothilone D has been accomplished. (S)-14-Methoxyepothilone D represents a conceptually novel example of polyketide analogue design based on an alternative biogenetic pattern of extender units. The significant biological activity observed for this compound provides a foundation to support studies designed to prepare derivatives of this type through fermentation of genetically engineered organisms expressing the epothilone PKS gene cluster.
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页码：3186 / 3189
页数：4
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