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Plant homeodomain (PHD) containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD finger 3 of KDM5A (KDM5A(PHD3)), a set of compounds were synthesised. Amiodarone and its derivatives were observed to weakly disrupt the interactions of a histone H3K4me3 peptide with KDM5A(PHD3). Selected amiodarone derivatives inhibited catalysis of KDM5A, but in a PHD-finger independent manner. Amiodarone derivatives also bind to H3K4me3-binding PHD-fingers from the KDM7 subfamily. Further work is required to develop potent and selective PHD finger inhibitors.

Original publication




Journal article


Bioorg Med Chem

Publication Date





2984 - 2991


Epigenetics, Histone demethylases, JmjC-KDMs, PHD-finger inhibitor, Plant Homeodomain, Amiodarone, Drug Delivery Systems, Drug Evaluation, Preclinical, Histone Demethylases, Histones, Lysine, Molecular Structure, Phylogeny, Plant Proteins, Protein Binding, Small Molecule Libraries