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Issue 12, 2014
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Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

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Abstract

G9a is a histone lysine methyltransferase (HKMT) involved in epigenetic regulation via the installation of histone methylation marks. 6,7-Dimethoxyquinazoline analogues, such as BIX-01294, are established as potent, substrate competitive inhibitors of G9a. With an objective to identify novel chemotypes for substrate competitive inhibitors of G9a, we have designed and synthesised a range of heterocyclic scaffolds, and investigated their ability to inhibit G9a. These studies have led to improved understanding of the key pharmacophoric features of BIX-01294 and the identification of a new core quinoline inhibitory scaffold, which retains excellent potency and high selectivity. Molecular docking was carried out to explain the observed in vitro data.

Graphical abstract: Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

  • This article is part of the themed collection: Epigenetics
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Publication details

The article was received on 24 Jun 2014, accepted on 25 Aug 2014 and first published on 26 Aug 2014


Article type: Concise Article
DOI: 10.1039/C4MD00274A
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Citation: Med. Chem. Commun., 2014,5, 1821-1828
  • Open access: Creative Commons BY license
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    Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

    N. Srimongkolpithak, S. Sundriyal, F. Li, M. Vedadi and M. J. Fuchter, Med. Chem. Commun., 2014, 5, 1821
    DOI: 10.1039/C4MD00274A

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