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Total synthesis of five thapsigargins: guaianolide natural products exhibiting sub-nanomolar SERCA inhibition.

Abstract:
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 further investigation of this phenomenon highlights the importance of these total syntheses. The first absolute stereochemical assignment of thapsivillosin C is also delineated.
Publication status:
Published

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Publisher copy:
10.1002/chem.200700302

Authors


Andrews, SP More by this author
Wierschem, F More by this author
Cleator, E More by this author
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Journal:
Chemistry (Weinheim an der Bergstrasse, Germany)
Volume:
13
Issue:
20
Pages:
5688-5712
Publication date:
2007
DOI:
EISSN:
1521-3765
ISSN:
0947-6539
URN:
uuid:f0805007-4809-44c4-a94b-fc9cef690424
Source identifiers:
58765
Local pid:
pubs:58765

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