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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
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Total synthesis and biological evaluation of histone deacetylase inhibitor WF-3161
Michael Kohr1, Niklas Papenkordt2, Manfred Jung2
1Organic Chemistry, Saarland University, D-66123 Saarbrücken, Germany. u.kazmaier@mx.uni-saarland.de.
Organic & Biomolecular Chemistry
|May 17, 2023
Abstract:
A novel synthesis of the naturally occurring HDAC inhibitor WF-3161 is described. Key steps include the Matteson homologation to generate the stereogenic centres in the side chain, and Pd-catalysed C-H functionalisation to connect the side chain to the peptide backbone. WF-3161 was found to be highly selective for HDAC1, whereas no activity was observed towards HDAC6. High activity was also found against the cancer cell line HL-60.
