Rapid Synthesis of New DNMT Inhibitors Derivatives of Procainamide (pages 157–165)
Ludovic Halby, Dr. Christine Champion, Catherine Sénamaud-Beaufort, Sophie Ajjan, Thierry Drujon, Arumugam Rajavelu, Dr. Alexandre Ceccaldi, Dr. Renata Jurkowska, Prof. Olivier Lequin, Dr. William G. Nelson, Prof. Alain Guy, Prof. Albert Jeltsch, Dr. Dominique Guianvarc'h, Prof. Clotilde Ferroud and Dr. Paola B. Arimondo
Version of Record online: 14 DEC 2011 | DOI: 10.1002/cbic.201100522
Rational inhibition: Conjugates of procainamide were produced by rapid synthetic pathways. Several compounds resulted in extremely potent inhibitors of the murine catalytic Dnmt3A/3L complex and of human DNMT1. The inhibition potency of procainamide conjugated to phtalimide depended on the length of the linker. Such conjugates also showed strong cytotoxicity against two tumour cell lines.