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  • Title: Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties.
    Author: Cosentino L, Redondo-Horcajo M, Zhao Y, Santos AR, Chowdury KF, Vinader V, Abdallah QM, Abdel-Rahman H, Fournier-Dit-Chabert J, Shnyder SD, Loadman PM, Fang WS, Díaz JF, Barasoain I, Burns PA, Pors K.
    Journal: J Med Chem; 2012 Dec 27; 55(24):11062-6. PubMed ID: 23176628.
    Abstract:
    Deacetylcolchicine was reacted with substituted benzyl halides to provide a library of compounds for biological analysis. Compound 7 (3,4-difluorobenzyl-N-aminocolchicine) was shown to possess cytotoxicity in cancer cell lines in the low nanomolar range. Significantly, it showed no loss of activity in the resistant A2780AD ovarian carcinoma cell line known to overexpress the ABCB1 drug transporter and was also unaffected by overexpression of class III β-tubulin in HeLa transfected cells.
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