These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation.
    Author: Fournier-Dit-Chabert J, Vinader V, Santos AR, Redondo-Horcajo M, Dreneau A, Basak R, Cosentino L, Marston G, Abdel-Rahman H, Loadman PM, Shnyder SD, Díaz JF, Barasoain I, Falconer RA, Pors K.
    Journal: Bioorg Med Chem Lett; 2012 Dec 15; 22(24):7693-6. PubMed ID: 23103097.
    Abstract:
    Colchicine was modified at the 10-OCH(3) position of the C-ring by reaction with heterocyclic amines or commercially available amines to afford a library of target colchicinoids in high yields (62-99%). Molecular modeling revealed that the incorporation of the linker groups led to a reduction in entropy and therefore binding affinity when compared with colchicine. Some colchicinoids were shown to be equicytotoxic with colchicine when evaluated in the DLD-1 colon cancer cells and retained activity in resistant A2780AD or HeLa cells with mutant Class III β-tubulin. Importantly, unlike colchicine, the analogues in this study are amenable for prodrug derivatisation and with potential for tumor-selective delivery.
    [Abstract] [Full Text] [Related] [New Search]