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Issue 12, 2013
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Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity

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Abstract

DNA-methyltransferases (DNMTs) are a class of epigenetic enzymes that catalyze the transfer of a methyl moiety from the methyl donor S-adenosyl-L-methionine onto the C5 position of cytosine in DNA. This process is dysregulated in cancers and leads to the hypermethylation and silencing of tumor suppressor genes. The development of potent and selective inhibitors of DNMTs is of utmost importance for the discovery of new therapies for the treatment of cancer. We report herein the synthesis and DNMT inhibitory activity of 29 analogues derived from NSC 319745. The effect of selected compounds on the methylation level in the MDA-MB-231 human breast cancer cell line was evaluated using a luminometric methylation assay. Molecular docking studies have been conducted to propose a binding mode for this series.

Graphical abstract: Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity

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Publication details

The article was received on 24 Jul 2013, accepted on 20 Sep 2013 and first published on 24 Sep 2013


Article type: Concise Article
DOI: 10.1039/C3MD00214D
Citation: Med. Chem. Commun., 2013,4, 1562-1570
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    Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity

    A. Kabro, H. Lachance, I. Marcoux-Archambault, V. Perrier, V. Doré, C. Gros, V. Masson, J. Gregoire, F. Ausseil, D. Cheishvili, N. B. Laulan, Y. St-Pierre, M. Szyf, P. B. Arimondo and A. Gagnon, Med. Chem. Commun., 2013, 4, 1562
    DOI: 10.1039/C3MD00214D

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