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Issue 8, 2012
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Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264

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Abstract

Three new bicyclic depsipeptides, which are related to the previously reported thailandepsins A (1), B (2) and C (3), were discovered from the culture broth of Burkholderia thailandensis E264 when supplemented with amino acid precursors, and were subsequently named as thailandepsins D (4), E (5) and F (6), respectively. Enzyme assays showed that 1–6 are potent histone deacetylase (HDAC) inhibitors, particularly toward HDAC1 which represents class I human HDACs.

Graphical abstract: Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264

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Publication details

The article was received on 30 Jan 2012, accepted on 20 Feb 2012 and first published on 22 Feb 2012


Article type: Concise Article
DOI: 10.1039/C2MD20024D
Citation: Med. Chem. Commun., 2012,3, 976-981
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    Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264

    C. Wang, C. J. Flemming and Y. Cheng, Med. Chem. Commun., 2012, 3, 976
    DOI: 10.1039/C2MD20024D

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