Mini-Reviews in Medicinal Chemistry

Author(s): Simon J. Shaw

DOI: 10.2174/138955708783744137

DownloadDownload PDF Flyer Cite As
The Structure Activity Relationship of Discodermolide Analogues

Page: [276 - 284] Pages: 9

  • * (Excluding Mailing and Handling)

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