Research Article
Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors
Published Online:8 Nov 2019https://doi.org/10.4155/fmc-2018-0587
Abstract
Aim: Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials & methods: A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities. Conclusion: Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.
Papers of special note have been highlighted as: • of interest; •• of considerable interest
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