Journal article
An azumamide C analogue without the zinc-binding functionality
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.
Language: | English |
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Year: | 2014 |
Pages: | 1849-1855 |
ISSN: | 20402511 and 20402503 |
Types: | Journal article |
DOI: | 10.1039/C4MD00252K |
ORCIDs: | 0000-0002-2953-8942 |