Format

Send to

Choose Destination
Eur J Med Chem. 2017 Jul 28;135:174-195. doi: 10.1016/j.ejmech.2017.04.013. Epub 2017 Apr 10.

Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.

Author information

1
SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
2
SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium. Electronic address: matthias.dhooghe@UGent.be.

Abstract

This paper provides an overview of the synthesis and biological activity of the most representative benzohydroxamic acid-based histone deacetylase inhibitors published to date. Benzohydroxamic acids comprise an important class of HDAC inhibitors, and recently several of these structures have been evaluated in clinical trials for the treatment of a variety of cancers. In this overview, benzohydroxamic acids were divided in four different classes based on their reported selectivity towards zinc-dependent HDACs: a first and major class consists of HDAC6 selective inhibitors, a second class deals with pan-HDAC inhibitors, a third class comprises HDAC8 selective inhibitors and a fourth, minor class includes dual HDAC6/8 selective inhibitors. Through this approach, structure-activity relationships were identified for each class, which could help future researchers in the design and development of novel benzohydroxamic acid-based HDAC inhibitors.

KEYWORDS:

Benzohydroxamic acid; HDAC6; HDAC8; Histone deacetylase inhibitor

PMID:
28453994
DOI:
10.1016/j.ejmech.2017.04.013
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center