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  • Title: B-ring-modified isocombretastatin A-4 analogues endowed with interesting anticancer activities.
    Author: Hamze A, Rasolofonjatovo E, Provot O, Mousset C, Veau D, Rodrigo J, Bignon J, Liu JM, Wdzieczak-Bakala J, Thoret S, Dubois J, Brion JD, Alami M.
    Journal: ChemMedChem; 2011 Dec 09; 6(12):2179-91. PubMed ID: 21990101.
    Abstract:
    A novel class of isocombretastatin A-4 (isoCA-4) analogues with modifications at the 3'-position of the B-ring by replacement with C-linked substituents was studied. Exploration of the structure-activity relationships of theses analogues led to the identification of several compounds that exhibit excellent antiproliferative activities in the nanomolar concentration range against H1299, MDA-MB231, HCT116, and K562 cancer cell lines; they also inhibit tubulin polymerization with potency similar to that of isoCA-4. 1,1-Diarylethylenes 8 and 17, respectively with (E)-propen-3-ol and propyn-3-ol substituents at the 3'-position of the B-ring, proved to be the most active in this series. Both compounds led to the arrest of various cancer cell lines at the G(2) /M phase of the cell cycle and strongly induced apoptosis. Docking of compounds 8 and 17 in the colchicine binding site indicated that their C3' substituents guide the positioning of the B-ring in a manner different from that observed for isoCA-4.
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