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© Yang SI, Institut Pasteur
Publication : Bioorganic & medicinal chemistry

Design and synthesis of new non nucleoside inhibitors of DNMT3A

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Bioorganic & medicinal chemistry - 10 Jul 2015

Erdmann A, Menon Y, Gros C, Molinier N, Novosad N, Samson A, Gregoire JM, Long C, Ausseil F, Halby L, Arimondo PB

Link to Pubmed [PMID] – 26220519

Bioorg. Med. Chem. 2015 Sep;23(17):5946-53

DNA methylation, an epigenetic modification regulating gene expression, is a promising target in cancer. In an effort to identify new non nucleosidic inhibitors of DNA methyltransferases, the enzymes responsible for DNA methylation, we carried out a high-throughput screening of 66,000 chemical compounds based on an enzymatic assay against catalytic DNMT3A. A family of propiophenone derivatives was identified. After chemical optimization and structure activity relationship studies, a new inhibitor (33) was obtained with an EC50 of 2.1 μM against DNMT3A. The mechanism of inhibition of the compound was investigated as it forms a reactive Michael acceptor group in situ. Thereby, the Michael acceptor 20 was identified. This compound was further characterized for its biological activity in cancer cells.

https://www.ncbi.nlm.nih.gov/pubmed/26220519