Synthesis and evaluation of analogues of N-phthaloyl-l-tryptophan (RG108) as inhibitors of DNA methyltransferase 1

…, C Senamaud-Beaufort, A Ceccaldi…

Index: Asgatay, Saaidia; Champion, Christine; Marloie, Gael; Drujon, Thierry; Senamaud-Beaufort, Catherine; Ceccaldi, Alexandre; Erdmann, Alexandre; Rajavelu, Arumugam; Schambel, Philippe; Jeltsch, Albert; Lequin, Olivier; Karoyan, Philippe; Arimondo, Paola B.; Guianvarc'H, Dominique Journal of Medicinal Chemistry, 2014 , vol. 57, # 2 p. 421 - 434

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Citation Number: 33

Abstract

DNA methyltransferases (DNMT) are promising drug targets in cancer provided that new, more specific, and chemically stable inhibitors are discovered. Among the non-nucleoside DNMT inhibitors, N-phthaloyl-l-tryptophan 1 (RG108) was first identified as inhibitor of DNMT1. Here, 1 analogues were synthesized to understand its interaction with DNMT. The indole, carboxylate, and phthalimide moieties were modified. Homologated and ...

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