Document Report Card
Basic Information
ID: ALA1143113
Journal: Bioorg Med Chem Lett
Title: 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.
Authors: Paquin I, Raeppel S, Leit S, Gaudette F, Zhou N, Moradei O, Saavedra O, Bernstein N, Raeppel F, Bouchain G, Fréchette S, Woo SH, Vaisburg A, Fournel M, Kalita A, Robert MF, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Rahil J, MacLeod AR, Besterman JM, Li Z, Delorme D.
Abstract: 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.
CiteXplore: 18160287