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  • New benzothieno[3,2-d]-1,2,...
    Lauria, Antonino; Alfio, Alessia; Bonsignore, Riccardo; Gentile, Carla; Martorana, Annamaria; Gennaro, Giuseppe; Barone, Giampaolo; Terenzi, Alessio; Almerico, Anna Maria

    Bioorganic & medicinal chemistry letters, 08/2014, Letnik: 24, Številka: 15
    Journal Article

    New benzothieno3,2-d-1,2,3-triazines, together with precursors triazenylbenzobthiophenes, were designed, synthesized and screened as anticancer agents. The structural features of these compounds prompted us to investigate their DNA binding capability through UV-vis absorption titrations, circular dichroism, and viscometry, pointing out the occurrence of groove-binding. The derivative 3-(4-methoxy-phenyl)benzothieno3,2-d-1,2,3-triazin-4(3H)-one showed the highest antiproliferative effect against HeLa cells and was also tested in cell cycle perturbation experiments. The obtained results assessed for the first time the anticancer activity of benzothieno3,2-d-1,2,3-triazine nucleus, and we related it to its DNA-binding properties.