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Issue 10, 2015
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Navigating into the chemical space between MGCD0103 and SAHA: novel histone deacetylase inhibitors as a promising lead

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Abstract

Histone deacetylase inhibitors (HDIs) are an increasingly important class of cancer-targeting agents. Two kinds of small molecule histone deacetylase inhibitors, mainly employing the motifs of the two known HDAC inhibitors MGCD0103 and SAHA as the basic scaffolds, were designed, synthesized and evaluated for the preliminary biological activity. Strikingly, these two compounds regained a long half-life potency like MGCD0103 and retained the non-selectivity for HDAC1 versus HDAC6 derived from SAHA. Together, these two compounds combining both the advantages of MGCD0103 and SAHA could be considered as novel histone deacetylase inhibitors in targeted drug development and possibly anticipated to be more effective under the clinical trials.

Graphical abstract: Navigating into the chemical space between MGCD0103 and SAHA: novel histone deacetylase inhibitors as a promising lead

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Supplementary files

Article information


Submitted
10 Jun 2015
Accepted
13 Aug 2015
First published
17 Aug 2015

Med. Chem. Commun., 2015,6, 1816-1825
Article type
Concise Article
Author version available

Navigating into the chemical space between MGCD0103 and SAHA: novel histone deacetylase inhibitors as a promising lead

X. Zhang, P. Lv, D. Li, W. Zhang and H. Zhu, Med. Chem. Commun., 2015, 6, 1816
DOI: 10.1039/C5MD00247H

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