Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity
| Autor: | Frédéric Ausseil, Jean-Marc Gregoire, Alexandre Gagnon, Anzhelika Kabro, Yves St-Pierre, Vicky Doré, Moshe Szyf, Véronique Masson, Hugo Lachance, Paola B. Arimondo, Christina Gros, Nathalie Bibens Laulan, Iris Marcoux-Archambault, David Cheishvili, Valérie Perrier |
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| Přispěvatelé: | Département de chimie [UdeM-Montréal], Université de Montréal (UdeM), Equipe PharmaQAM - Département de Chimie et de Biochimie, Université du Québec à Montréal = University of Québec in Montréal (UQAM), Pharmacochimie de la Régulation Epigénétique du Cancer (ETaC), PIERRE FABRE-Centre National de la Recherche Scientifique (CNRS), Institut Armand Frappier (INRS-IAF), Institut National de la Recherche Scientifique [Québec] (INRS)-Réseau International des Instituts Pasteur (RIIP), Department of Pharmacology and Therapeutics [Montréal], McGill University = Université McGill [Montréal, Canada] |
| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: |
Pharmacology
chemistry.chemical_classification [SDV]Life Sciences [q-bio] Organic Chemistry Pharmaceutical Science Cancer Methylation medicine.disease Biochemistry chemistry.chemical_compound Enzyme chemistry Drug Discovery DNA methylation medicine Molecular Medicine Gene silencing Epigenetics Cytosine DNA |
| Zdroj: | MedChemComm MedChemComm, Royal Society of Chemistry, 2013, 4 (12), pp.1562-1570. ⟨10.1039/C3MD00214D⟩ |
| ISSN: | 2040-2503 2040-2511 |
| Popis: | International audience; 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 |
| Databáze: | OpenAIRE |
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