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Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors

2007; Elsevier BV; Volume: 18; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2007.12.009

1464-3405

Isabelle Paquin, Stéphane Raeppel, Silvana Leit, Frédéric Gaudette, Nancy Zhou, Oscar Moradei, Oscar Saavedra, Naomy Bernstein, Franck Raeppel, Giliane Bouchain, Sylvie Fréchette, Soon Hyung Woo, Arkadii Vaisburg, Marielle Fournel, Ann Kalita, Marie‐France Robert, Aihua Lu, Marie-Claude Trachy-Bourget, Pu Yan, Jianhong Liu, Jubrail Rahil, A. Robert MacLeod, Jeffrey M. Besterman, Zuomei Li, Daniel Delorme,

Adenosine and Purinergic Signaling

Inhibition of histone deacetylases (HDAC) is emerging as a new strategy in human cancer therapy. The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides is presented herein. From the different series bearing a six-membered heteroaromatic ring studied, the s-triazine series showed the best HDAC1 enzyme and in vitro anti-proliferative activities with IC(50) values below micromolar range. Some of these compounds can also significantly reduce tumor growth in human tumor xenograft models in mice.