Total synthesis of five thapsigargins:: Guaianolide natural products exhibiting sub-nanomolar SERCA inhibition
Total synthesis of five thapsigargins:: Guaianolide natural products exhibiting sub-nanomolar SERCA inhibition
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DOI：
10.1002/chem.200700302
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发表时间：
2007-01-01
影响因子：
4.3
通讯作者：
Ley, Steven V.
中科院分区：
文献类型：
--
作者：
Andrews, Stephen P.;Ball, Matthew;Ley, Steven V.
本文介绍了五种愈创木酚素天然产物：毒胡萝卜素、毒胡萝卜素C、毒胡萝卜素F、三叶草素和去甲三叶草素的全合成。毒胡萝卜素的前药衍生物已经显示出对前列腺肿瘤的选择性体内细胞毒性，并且这种现象的需要突出了这些全合成的重要性。第一个绝对的立体化学分配thapsivillosin C也划定。
Herein we describe the total synthesis of five guaianolide natural products: thapsigargin, thapsivillosin C, thapsivillosin F, trilobolide and nortrilobolide. Prodrug derivatives of thapsigargin have shown selective in vivo cytotoxicity against prostate tumours and the need for of this phenomenon highlights the importance of these total syntheses. The first absolute stereochemical assignment of thapsivillosin C is also delineated.