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Pubmed ID :26741168
Publication Date : //

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.


We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors which bind to Fe(II) in the active site. Substitution from C4 of the pyrazole moiety allows access to the histone peptide substrate binding site; incorporation of a conformationally constrained 4-phenylpiperidine linker gives derivatives such as 54j and 54k which demonstrate equipotent activity versus the KDM4 (JMJD2) and KDM5 (JARID1) subfamily demethylases, selectivity over representative exemplars of the KDM2, KDM3, and KDM6 subfamilies, cellular permeability in the Caco-2 assay, and, for 54k, inhibition of H3K9Me3 and H3K4Me3 demethylation in a cell-based assay.

Authors : Bavetsias Vassilios , Lanigan Rachel M , Ruda Gian Filippo , Atrash Butrus , McLaughlin Mark G , Tumber Anthony , Mok N Yi , Le Bihan Yann-Vaï , Dempster Sally , Boxall Katherine J , Jeganathan Fiona , Hatch Stephanie B , Savitsky Pavel , Velupillai Srikannathasan , Krojer Tobias , England Katherine S , Sejberg Jimmy , Thai Ching , Donovan Adam , Pal Akos , Scozzafava Giuseppe , Bennett James M , Kawamura Akane , Johansson Catrine , Szykowska Aleksandra , Gileadi Carina , Burgess-Brown Nicola A , von Delft Frank , Oppermann Udo , Walters Zoe , Shipley Janet , Raynaud Florence I , Westaway Susan M , Prinjha Rab K , Fedorov Oleg , Burke Rosemary , Schofield Christopher J , Westwood Isaac M , Bountra Chas , Müller Susanne , van Montfort Rob L M , Brennan Paul E , Blagg Julian ,

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