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The Structure Activity Relationship of Discodermolide Analogues

[ Vol. 8 , Issue. 3 ]

Author(s):

Simon J. Shaw   Pages 276 - 284 ( 9 )

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

Affiliation:

Kosan Biosciences, Inc. 3832 Bay Center Place, Hayward, CA 94545, USA.



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