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  • Title: Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors.
    Author: Audisio D, Methy-Gonnot D, Radanyi C, Renoir JM, Denis S, Sauvage F, Vergnaud-Gauduchon J, Brion JD, Messaoudi S, Alami M.
    Journal: Eur J Med Chem; 2014 Aug 18; 83():498-507. PubMed ID: 24992077.
    Abstract:
    A series of substituted coumarins1-10 was designed and synthesized as a novel class of 4TCNA analogues. Compound 2a showed excellent antiproliferative activity with mean GI50 values at a micromolar level in a diverse set of human cancer cells (GI50 = 2-30 μM) and induced a high apoptosis level in MCF-7 breast cancer cell line. The molecular signature of hsp90 inhibition was assessed by depletion of the Erα hsp90 client protein.
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