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© Yang SI, Institut Pasteur
Publication : European journal of medicinal chemistry

Synthesis of novel 3-halo-3-nitroflavanones and their activities as DNA methyltransferase inhibitors in cancer cells

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in European journal of medicinal chemistry - 01 Nov 2019

Pechalrieu D, Dauzonne D, Arimondo PB, Lopez M

Link to Pubmed [PMID] – 31757526

Eur J Med Chem 2020 Jan;186:111829

The implication of DNA methylation in cancer is today clearly established. Despite that nucleoside analogues are currently used for leukaemia treatment, their low stability in physiological conditions and their lack of selectivity arise the need for the identification of non-nucleoside DNA methyltransferase inhibitors. Here, we describe the synthesis and pharmacological characterisation of a novel class of DNA methyltransferase inhibitors: the 3-halo-3-nitroflavanones. We showed that 3-bromo-3-nitroflavanones 3b and 4a have a micromolar DNMT inhibition and an increased potency in a cell reporter model. Interestingly they are significantly more stable than the reference compounds and induce a low cytotoxicity, supporting them as new candidates for the development of non-cytotoxic cell-reprogramming epi-drugs for anticancer treatment.

https://www.ncbi.nlm.nih.gov/pubmed/31757526