The Structure Activity Relationship of Discodermolide Analogues

Simon   J.   Shaw

doi:10.2174/138955708783744137

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

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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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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