Total Synthesis and Biological Evaluation of Apratoxin E and Its C30 Epimer: Configurational Reassignment of the Natural Product.
Total Synthesis and Biological Evaluation of Apratoxin E and Its C30 Epimer: Configurational Reassignment of the Natural Product.
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Apratoxin E 及其 C30 差向异构体的全合成和生物学评价：天然产物的构型重新分配。
DOI：
10.1021/acs.orglett.6b02780
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发表时间：
2016-10-21
期刊：
影响因子：
5.2
通讯作者：
Luesch H
中科院分区：
文献类型：
--
作者：
Wu P;Cai W;Chen QY;Xu S;Yin R;Li Y;Zhang W;Luesch H
Apratoxin E 为临床前开发中的 apratoxin A/E 杂合体的设计提供了灵感。通过使用两种不同策略的全合成，确定了最初提出的 C30 处噻唑啉的构型与 apratoxin A 中的构型相反，这与之前对生物合成的假设相反。合成了差向异构体和真正的天然阿普拉毒素E，并评价了其生物活性。
Apratoxin E provided the inspiration for the design of apratoxin A/E hybrids under preclinical development. Through total synthesis using two different strategies, it was determined that the originally proposed configuration of the thiazoline at C30 is opposite from that in apratoxin A, in contrast to previous assumptions on biosynthetic grounds. The epimer and true natural apratoxin E were synthesized, and the biological activities were evaluated.