Bioorganic & Medicinal Chemistry 26 (2018) 2984–2991 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-ﬁnger of JmjC histone demethylases a,b,e a,e a a a,c Bhaskar Bhushan , Alexandre Erdmann , Yijia Zhang , Roman Belle , Catrine Johannson , c a,d a a,b,⇑ Udo Oppermann , Richard J. Hopkinson , Christopher J. Schoﬁeld , Akane Kawamura Department of Chemistry, University of Oxford, Mansﬁeld Road, Oxford OX1 3TA, United Kingdom Radcliffe Department of Medicine, Division of Cardiovascular Medicine, University of Oxford, The Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Oxford OX3 7BN, United Kingdom Botnar Research Centre, NIHR Oxford Biomedical Research Unit, University of Oxford, Oxford, United Kingdom ar ti c l e i nf o ab stra ct Article history: Plant homeodomain (PHD) ﬁnger containing proteins are important epigenetic regulators and are of Received 15 February 2018 interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD Revised 10 March 2018 ﬁnger 3 of KDM5A (KDM5A(PHD3)), a set of compounds were synthesised. Amiodarone and its Accepted 18 March 2018 derivatives were observed to weakly disrupt the interactions
Bioorganic & Medicinal Chemistry – Elsevier
Published: Jul 15, 2018
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