An azumamide C analogue without the zinc-binding functionality

Jesper Villadsen, Betül Kitir, Kathrine Wich, Tina Friis, Andreas Stahl Madsen, Christian Adam Olsen

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Histone deacetylase (HDAC) inhibitors have attracted considerable attention due to their promise as therapeutic agents. Most HDAC inhibitors adhere to a general “ cap-linker-Zn 2+ -binding group ” architecture but recent studies have indicated that potent inhibition may be achieved without a Zn 2+ - coordinating moiety. Herein, we describe the synthesis of an azumamide analogue lacking its native Zn 2+ -binding group and evaluation of its inhibitory activity against recombinant human HDAC1 – 11. Furthermore, kinetic investigation of the inhibitory mechanism of both parent natural product and synthetic analogue against HDAC3-NCoR2 is reported as well as their activity against Burkitt's lymphoma cell proliferation.
Original languageEnglish
Pages (from-to)1849-1855
Publication statusPublished - 2014


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