Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability

Benelkebir, Hanae, Marie, Sabrina, Hayden, Annette L., Lyle, Jason, Loadman, Paul M., Crabb, Simon J., Packham, Graham and Ganesan, A (2011) Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. Bioorganic & Medicinal Chemistry, 19 (12). pp. 3650-3658.

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Abstract

The total synthesis of largazole and four analogues is reported. All analogues were nanomolar HDAC inhibitors. The antiproliferative activity is driven by lipophilicity and cell permeability. In murine liver homogenates, largazole is rapidly metabolized (half-life ?5 min) to the thiol which has a half-life of 51 min.

Item Type:	Article
Faculty \ School:	Faculty of Science > School of Pharmacy (former - to 2024)
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:	Users 2731 not found.
Date Deposited:	20 Oct 2011 10:43
Last Modified:	28 Mar 2025 02:44
URI:	https://ueaeprints.uea.ac.uk/id/eprint/35105
DOI:	10.1016/j.bmc.2011.02.024

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