Title of article
Natural products as starting materials for development of second-generation SERCA inhibitors targeted towards prostate cancer cells Original Research Article
Author/Authors
Helmer S?hoel، نويسنده , , Anne-Marie Lund Jensen، نويسنده , , Jesper V. M?ller، نويسنده , , Poul Nissen، نويسنده , , Samuel R. Denmeade، نويسنده , , John T. Isaacs، نويسنده , , Carl Erik Olsen، نويسنده , , S. Br?gger Christensen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
2810
To page
2815
Abstract
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 on 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.
Keywords
SERCA inhibitors , X-ray structure , Synthesis , Thapsigargin
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305652
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