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Bioorg Chem. 2015 Apr;59:145-50. doi: 10.1016/j.bioorg.2015.02.009. Epub 2015 Mar 7.

An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.

Author information

1
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan; Department of Chemistry, Faculty of Science, University of Rajshahi, Rajshahi 6205, Bangladesh. Electronic address: shahidulchem@yahoo.com.
2
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan; Department of Chemistry, Faculty of Science, University of Rajshahi, Rajshahi 6205, Bangladesh.
3
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan; Department of Biochemistry and Molecular Biology, Faculty of Science, University of Rajshahi, Rajshahi 6205, Bangladesh.
4
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan.
5
BioRunxInc., Seoul 110-749, Republic of Korea.
6
Chemical Genetics Laboratory/Chemical Genomics Research Group, RIKEN Advanced Science Institute, Saitama 351-0198, Japan.

Abstract

SK-658 is a potent histone deacetylase (HDAC) inhibitor that showed higher activity than SAHA due to the presence of extended hydrophobic group. We designed and synthesized thioester and SS-hybrid bearing SK-658 analogs as HDAC inhibitors. All the compounds were active in nano molar range and showed higher inhibitory activity than SAHA and SK-658. Among these, disulfide compounds showed the highest activity.

KEYWORDS:

Histone deacetylase inhibitor; SK-658 analogs; SS-hybrid; Zinc binding group

PMID:
25797804
DOI:
10.1016/j.bioorg.2015.02.009
[Indexed for MEDLINE]

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