Abstract
The marine polyketide discodermolide is a member of a class of natural products that stabilize microtubules. Many analogues have been synthesized suggesting that few changes can be made to the internal carbon backbone. Both ends of the molecule, however, can be modified. The majority of analogues have been generated via modification of the lactone region. This suggests that significant simplifications can be made in this region provided that the lactone moiety is maintained.
Keywords: lactone ring, Dictyostatin, pharmacokinetics, MDR cell line, SAR
Mini-Reviews in Medicinal Chemistry
Title: The Structure Activity Relationship of Discodermolide Analogues
Volume: 8 Issue: 3
Author(s): Simon J. Shaw
Affiliation:
Keywords: lactone ring, Dictyostatin, pharmacokinetics, MDR cell line, SAR
Abstract: The marine polyketide discodermolide is a member of a class of natural products that stabilize microtubules. Many analogues have been synthesized suggesting that few changes can be made to the internal carbon backbone. Both ends of the molecule, however, can be modified. The majority of analogues have been generated via modification of the lactone region. This suggests that significant simplifications can be made in this region provided that the lactone moiety is maintained.
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Cite this article as:
Shaw J. Simon, The Structure Activity Relationship of Discodermolide Analogues, Mini-Reviews in Medicinal Chemistry 2008; 8 (3) . https://dx.doi.org/10.2174/138955708783744137
DOI https://dx.doi.org/10.2174/138955708783744137 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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