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

Carole Seidel; Michael Schnekenburger; Clemens Zwergel; François Gaascht; Antonello Mai; Mario Dicato; Gilbert Kirsch; Sergio Valente; Marc Diederich

doi:10.1016/j.bmcl.2014.06.067

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

Carole Seidel, Michael Schnekenburger, Clemens Zwergel, François Gaascht, Antonello Mai, Mario Dicato, Gilbert Kirsch, Sergio Valente, Marc Diederich

Biotechnology Institute

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

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.

Original language	English (US)
Pages (from-to)	3797-3801
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	16
DOIs	https://doi.org/10.1016/j.bmcl.2014.06.067
State	Published - Aug 15 2014

Keywords

Anti-proliferative activity
Cancer
Chalcone
Coumarin
Histone deacetylase inhibitors

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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

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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AU - Seidel, Carole

AU - Schnekenburger, Michael

AU - Zwergel, Clemens

AU - Gaascht, François

AU - Mai, Antonello

AU - Dicato, Mario

AU - Kirsch, Gilbert

AU - Valente, Sergio

AU - Diederich, Marc

PY - 2014/8/15

Y1 - 2014/8/15

N2 - 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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KW - Anti-proliferative activity

KW - Cancer

KW - Chalcone

KW - Coumarin

KW - Histone deacetylase inhibitors

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DO - 10.1016/j.bmcl.2014.06.067

M3 - Article

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

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

Abstract

Keywords

UN SDGs

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