Total synthesis and stereochemical assignment of burkholdac B, a depsipeptide HDAC inhibitor

Benelkebir, Hanae, Donlevy, Alison M., Packham, Graham and Ganesan, A. ORCID: https://orcid.org/0000-0003-4862-7999 (2011) Total synthesis and stereochemical assignment of burkholdac B, a depsipeptide HDAC inhibitor. Organic Letters, 13 (24). pp. 6334-6337. ISSN 1523-7060

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Abstract

Three diastereomers of burkholdac B were prepared by total synthesis, enabling the full stereochemical assignment of the natural product. It is proposed that burkholdac B is identical to thailandepsin A independently isolated by Cheng from the same strain of Burkholderia thailandensis. Burkholdac B is the most potent among depsipeptide histone deacetylase inhibitors in growth inhibition of the MCF7 breast cancer cell line with an IC50 of 60 pM. © 2011 American Chemical Society.

Item Type: Article
Uncontrolled Keywords: sdg 3 - good health and well-being ,/dk/atira/pure/sustainabledevelopmentgoals/good_health_and_well_being
Faculty \ School: Faculty of Science > School of Pharmacy
UEA Research Groups: Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017)
Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021)
Depositing User: Rhiannon Harvey
Date Deposited: 14 Mar 2012 15:16
Last Modified: 23 Jan 2024 01:20
URI: https://ueaeprints.uea.ac.uk/id/eprint/38291
DOI: 10.1021/ol202197q

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