| Literature DB >> 26771203 |
Susan M Westaway1, Alex G S Preston1, Michael D Barker1, Fiona Brown2, Jack A Brown1, Matthew Campbell1, Chun-wa Chung2, Gerard Drewes3, Robert Eagle2, Neil Garton1, Laurie Gordon2, Carl Haslam2, Thomas G Hayhow1, Philip G Humphreys1, Gerard Joberty3, Roy Katso2, Laurens Kruidenier1, Melanie Leveridge2, Michelle Pemberton2, Inma Rioja1, Gail A Seal1, Tracy Shipley1, Onkar Singh2, Colin J Suckling4, Joanna Taylor2, Pamela Thomas2, David M Wilson1, Kevin Lee1, Rab K Prinjha1.
Abstract
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.Entities:
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Year: 2016 PMID： 26771203 DOI： 10.1021/acs.jmedchem.5b01538
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446