Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 14, Pages 3201-3204Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.05.002
Keywords
KDM4D; Histone lysine demethylase; Epigenetics; Small molecule inhibitor; Structure-activity relationship
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Funding
- 973 Program [2013CB967204]
- National Natural Science Foundation of China [81325021, 81473140, 81573349]
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Herein we report the discovery of a series of new small molecule inhibitors of histone lysine demethylase 4D (KDM4D). Molecular docking was first performed to screen for new KDM4D inhibitors from various chemical databases. Two hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the more selective one, compound 2, which led to the discovery of several new KDM4D inhibitors. Among them, compound 10r is the most potent one with an IC50 value of 0.41 +/- 0.03 mu M against KDM4D. Overall, compound 10r could be taken as a good lead compound for further studies. (C) 2017 Published by Elsevier Ltd.
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