Total synthesis and biological evaluation of histone deacetylase inhibitor WF-3161.

Michael Kohr, Niklas Papenkordt, Manfred Jung, Uli Kazmaier

Organic & biomolecular chemistry 2023 May 31

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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.

Citation

Michael Kohr, Niklas Papenkordt, Manfred Jung, Uli Kazmaier. Total synthesis and biological evaluation of histone deacetylase inhibitor WF-3161. Organic & biomolecular chemistry. 2023 May 31;21(21):4382-4387