Antimitotic eleuthesides

Details Antimitotic eleuthesides Antimitotic eleuthesides

C - Chemistry, Metallurgy

07

H

C07H 15/26 (2006.01) C07H 17/02 (2006.01)

Patent

CA 2451511

This invention provides analogs of eleutherobin and the eleuthesides modified at the C-11 position or comprising an epoxide functionality from C-11 to C-12. C-11 to C-12 is an ideal location for conjugating functional moieties to the eleutherobin pharmacophore without significant loss of antimitotic activity. Moieties that may be conjugated at C-11 include those intended to increase the solubility of the pharmacophore, to facilitate drug formulation, or to facilitate in vivo delivery or targeting.

L'invention concerne des analogues de l'éleuthérobine et les éleuthésides modifiés sur la position C-11 ou comprenant une fonctionnalité époxyde de C-11 à C-12. C-11 à C-12 est un emplacement idéal pour conjuguer des fragments fonctionnels au pharmacophore de l'éleuthérobine sans perte significative d'activité antimitotique. Les fragments pouvant être conjugués sur C-11 comprennent ceux destinés à augmenter la solubilité du pharmacophore, afin de faciliter la formulation de médicaments, ou afin de faciliter l'administration ou le ciblage in vivo.

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