Multimodal HDAC Inhibitors with Improved Anticancer Activity

Author(s): Rainer Schobert, Bernhard Biersack*

Journal Name: Current Cancer Drug Targets

Volume 18 , Issue 1 , 2018

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Graphical Abstract:


Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.

Keywords: Anticancer drugs, epigenetics, histone deacetylases, kinases, DNA targeting, HDAC inhibitors, hybrid molecules.

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Article Details

Year: 2018
Published on: 05 February, 2017
Page: [39 - 56]
Pages: 18
DOI: 10.2174/1568009617666170206102613
Price: $65

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