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

…, V Poughon??Cassabois, A Rajavelu, A Jeltsch…

Index: Rilova, Elodie; Erdmann, Alexandre; Gros, Christina; Masson, Veronique; Aussagues, Yannick; Poughon-Cassabois, Valerie; Rajavelu, Arumugam; Jeltsch, Albert; Menon, Yoann; Novosad, Natacha; Gregoire, Jean-Marc; Vispe, Stephane; Schambel, Philippe; Ausseil, Frederic; Sautel, Francois; Arimondo, Paola B.; Cantagrel, Frederic ChemMedChem, 2014 , vol. 9, # 3 p. 590 - 601

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Citation Number: 14

Abstract

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 ...