Issue 8, 2012

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

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

Supplementary files

Article information

Article type
Concise Article
Submitted
30 Jan 2012
Accepted
20 Feb 2012
First published
22 Feb 2012

Med. Chem. Commun., 2012,3, 976-981

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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