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Total synthesis of five thapsigargins: guaianolide natural products exhibiting sub-nanomolar SERCA inhibition |
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| Authors: | Andrews Stephen P Ball Matthew Wierschem Frank Cleator Ed Oliver Steven Högenauer Klemens Simic Oliver Antonello Alessandra Hünger Udo Smith Martin D Ley Steven V |
| Affiliation: | University Chemical Laboratory, Lensifield Road, Cambridge, CB2 1EW, UK. |
| 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. |
| Keywords: | guaianolide natural products sesquiterpene thapsigargin total synthesis |
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