The Structure Activity Relationship of Discodermolide Analogues

Author(s): Simon J. Shaw.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 8 , Issue 3 , 2008

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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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Article Details

VOLUME: 8
ISSUE: 3
Year: 2008
Page: [276 - 284]
Pages: 9
DOI: 10.2174/138955708783744137
Price: $58

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