Bioorganic & Medicinal Chemistry 26 (2018) 3021–3029 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc Synthesis and proﬁling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identiﬁcation of 3-amino-5-(pyridin-4-yl)pyridin-2 (1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition a a a b a,⇑ Daren Fearon , Isaac M. Westwood , Rob L.M. van Montfort , Richard Bayliss , Keith Jones , a,⇑ Vassilios Bavetsias Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London SM2 5NG, UK Astbury Centre for Structural Molecular Biology, School of Molecular and Cellular Biology, Faculty of Biological Sciences, University of Leeds, UK article i nfo abstract Article history: Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the Received 31 January 2018 human kinome identiﬁed 3-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5- Revised 13 April 2018 (pyridin-4-yl)pyridin-2(1H)-one (3) as ligand efﬁcient inhibitors of the mitotic kinase Monopolar Accepted 15 April 2018 Spindle 1 (MPS1) and the Aurora kinase family. These kinases are well recognised as attractive targets Available online 17 April 2018 for therapeutic intervention for treating cancer. Elucidation of the binding mode of these fragments and their analogues has been carried out by X-ray crystallography.
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