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Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity

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
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https://hal-riip.archives-ouvertes.fr/pasteur-01133260
Contributor : Michel Courcelles <>
Submitted on : Wednesday, March 18, 2015 - 7:55:32 PM
Last modification on : Monday, August 31, 2020 - 4:34:04 PM

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Anzhelika Kabro, Hugo Lachance, Iris Marcoux-Archambault, Valérie Perrier, Vicky Doré, et al.. Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity. MedChemComm, Royal Society of Chemistry, 2013, 4 (12), pp.1562-1570. ⟨10.1039/C3MD00214D⟩. ⟨pasteur-01133260⟩

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