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N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors

2007; Elsevier BV; Volume: 17; Issue: 24 Linguagem: Inglês

10.1016/j.bmcl.2007.10.050

1464-3405

Arkadii Vaisburg, Isabelle Paquin, Naomy Bernstein, Sylvie Fréchette, Frédéric Gaudette, Silvana Leit, Oscar Moradei, Stéphane Raeppel, Nancy Zhou, Giliane Bouchain, Soon Hyung Woo, Zhiyun Jin, J. H. Gillespie, Jinru Wang, Marielle Fournel, Pu Yan, Marie-Claude Trachy-Bourget, Marie‐France Robert, Aihua Lu, Jimmy Yuk, Jubrail Rahil, A. Robert MacLeod, Jeffrey M. Besterman, Zuomei Li, Daniel Delorme,

Peptidase Inhibition and Analysis

A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides were designed and synthesized. These compounds were shown to inhibit recombinant human HDAC1 with IC50 values in the sub-micromolar range. In human cancer cells growing in culture these compounds induced hyperacetylation of histones, induced the expression of the tumor suppressor protein p21WAF1/Cip1, and inhibited cellular proliferation. Certain compounds of this class also showed in vivo activity in various human tumor xenograft models in mice.