Design, synthesis and biological evaluation of pyrazole derivatives as potential multi-kinase inhibitors in hepatocellular carcinoma

…, E Locatelli, L Bolondi, M Comes-Franchini

文献索引：Strocchi, Elena; Fornari, Francesca; Minguzzi, Manuela; Gramantieri, Laura; Milazzo, Maddalena; Rebuttini, Valentina; Breviglieri, Simone; Camaggi, Carlo Maurizio; Locatelli, Erica; Bolondi, Luigi; Comes-Franchini, Mauro European Journal of Medicinal Chemistry, 2012 , vol. 48, p. 391 - 401

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被引用次数: 15

摘要

We described the optimization, by molecular modelling, of small pyrazole derivatives, as kinase inhibitors, obtained through a 1, 3-dipolar cycloaddition between nitrile imines and functionalized acetylenes. The two compounds, selected as potential agents active against hepatocellular carcinoma (HCC) were then evaluated in vitro for their biological activity on HCC-derived cell lines. The compounds show a promising inhibitory growth efficacy (IC50 ...