Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 8, Pages 2810-2815Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.12.001
Keywords
SERCA inhibitors; X-ray structure; synthesis; thapsigargin
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An analysis of the binding of the 8-O-N-tert-butoxycarbonyl-12-aminododecanoyl derivative of 8-O-debutanoylthapsigargin to the target molecule, the SERCA pump, has revealed the importance of the length and flexibility of the side chain attached to O-8. Based oil the analysis a series of analogues to the 2-unsubstituted analogue trilobolide has been constructed and shown to be equipotent with thapsigargin as SERCA inhibitors. Only the 12-Boc-aminododecaonoyl derivative, however, was found to be apoptotic. (c) 2005 Elsevier Ltd. All rights reserved.
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