Design and total synthesis of unnatural analogues of the sub-nanomolar SERCA inhibitor thapsigargin

被引：14

作者：

Andrews, Stephen P.

Tait, Malcolm M.

Ball, Matthew

Ley, Steven V.

机构：

[1] Univ Cambridge, Chem Lab, Cambridge CB2 1EW, England

[2] GlaxoSmithKline Inc, GI Med Chem Neurol & GICEDD, Harlow CM19 5AW, Essex, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2007年 / 5卷 / 09期

关键词：

D O I：

10.1039/b702481a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Thapsigargin is a densely oxygenated guaianolide which displays potent sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) binding affinities. The total syntheses of designed unnatural analogues of this important natural product are described. This article constitutes the chemical synthesis behind an ongoing project. Rational modi. cations have been made to the lactone region of thapsigargin in order to obtain derivatives for future structure - activity relationship studies.

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页码：1427 / 1436

页数：10

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