Design, Synthesis and Biological Evaluation of 4-Amino-N-(4-aminophenyl)benzamide Analogues of Quinoline-Based SGI-1027 as Inhibitors of DNA Methylation

@inproceedings{Rilova2014DesignSA,
  title={Design, Synthesis and Biological Evaluation of 4-Amino-N-(4-aminophenyl)benzamide Analogues of Quinoline-Based SGI-1027 as Inhibitors of DNA Methylation},
  author={Elodie Rilova and Alexandre Erdmann and Christina Gros and V{\'e}ronique Masson and Yannick Aussagues and Val{\'e}rie Poughon-Cassabois and Arumugam Rajavelu and Albert Jeltsch and Yoann Menon and Natacha Novosad and Jean-Marc Gregoire and St{\'e}phane Visp{\'e} and Philippe Schambel and Fr{\'e}d{\'e}ric Ausseil and François Sautel and Paola B. Arimondo and Fr{\'e}d{\'e}ric Cantagrel},
  booktitle={ChemMedChem},
  year={2014}
}
Quinoline derivative SGI-1027 (N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide) was first described in 2009 as a potent inhibitor of DNA methyltransferase (DNMT) 1, 3A and 3B. Based on molecular modeling studies, performed using the crystal structure of Haemophilus haemolyticus cytosine-5 DNA methyltransferase (MHhaI C5 DNMT), which suggested that the quinoline and the aminopyridimine moieties of SGI-1027 are important for interaction with the substrates and… CONTINUE READING