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Novel inhibitors of human histone deacetylases: Design, synthesis and bioactivity of 3-alkenoylcoumarines

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Abstract

Histone deacetylases (HDACs) are well-established, promising targets for anticancer therapy due to their critical role in cancer development. Accordingly, an increasing number of HDAC inhibitors displaying cytotoxic effects against cancer cells have been reported. Among them, a large panel of chemical structures was described including coumarin-containing molecules. In this study, we described synthesis and biological activity of new coumarin-based derivatives as HDAC inhibitors. Among eight derivatives, three compounds showed HDAC inhibitory activities and antitumor activities against leukemia cell lines without affecting the viability of peripheral blood mononuclear cells from healthy donors. © 2014 Elsevier Ltd. All rights reserved.

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Seidel, C., Schnekenburger, M., Zwergel, C., Gaascht, F., Mai, A., Dicato, M., … Diederich, M. (2014). Novel inhibitors of human histone deacetylases: Design, synthesis and bioactivity of 3-alkenoylcoumarines. Bioorganic and Medicinal Chemistry Letters, 24(16), 3797–3801. https://doi.org/10.1016/j.bmcl.2014.06.067

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