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

Authors
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Aug 23, 2014
Volume
24
Issue
16
Pages
3801–3801
Identifiers
DOI: 10.1016/j.bmcl.2014.06.067
Source
LBMCC
Keywords
License
Green

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.

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