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Rapid synthesis of new DNMT inhibitors derivatives of procainamide

Halby, Ludovic, Champion, Christine, Sénamaud-Beaufort, Catherine, Ajjan, Sophie, Drujon, Thierry, Rajavelu, Arumugam, Ceccaldi, Alexandre, Jurkowska, Renata ORCID:, Lequin, Olivier, Nelson, William G., Guy, Alain, Jeltsch, Albert, Guianvarc'h, Dominique, Ferroud, Clotilde and Arimondo, Paola B. 2012. Rapid synthesis of new DNMT inhibitors derivatives of procainamide. ChemBioChem 13 (1) , pp. 157-165. 10.1002/cbic.201100522

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DNA methyltransferases (DNMTs) are responsible for DNA methylation, an epigenetic modification involved in gene regulation. Families of conjugates of procainamide, an inhibitor of DNMT1, were conceived and produced by rapid synthetic pathways. Six compounds resulted in potent inhibitors of the murine catalytic Dnmt3A/3L complex and of human DNMT1, at least 50 times greater than that of the parent compounds. The inhibitors showed selectivity for C5 DNA methyltransferases. The cytotoxicity of the inhibitors was validated on two tumour cell lines (DU145 and HCT116) and correlated with the DNMT inhibitory potency. The inhibition potency of procainamide conjugated to phthalimide through alkyl linkers depended on the length of the linker; the dodecane linker was the best.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Publisher: Wiley
ISSN: 1439-4227
Last Modified: 09 Nov 2022 10:22

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