4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.


The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs is described. Some of these compounds were shown to inhibit HDAC1 with IC(50) values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21(WAF1/Cip1), and inhibit proliferation of human cancer cells. In addition, certain compounds of this class were active in several human tumor xenograft models in vivo.

DOI: 10.1016/j.bmcl.2007.12.057

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@article{Frchette20084HeteroarylaminomethylN2aminophen, title={4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.}, author={Sylvie Fr{\'e}chette and Silvana M Leit and Soon Hyung Woo and Guillaume Lapointe and Guillaume Jeannotte and Oscar M Moradei and Isabelle Paquin and Giliane Bouchain and St{\'e}phane L. Raeppel and Fr{\'e}d{\'e}ric Gaudette and Nancy Z Zhou and Arkadii F Vaisburg and Marielle Fournel and Pu Theresa Yan and Marie-Claude Trachy-Bourget and Ann M Kalita and Marie-France Robert and Aihua Lu and Jubrail Rahil and A Robert Macleod and Jeffrey M. Besterman and Zuomei Li and Daniel Delorme}, journal={Bioorganic & medicinal chemistry letters}, year={2008}, volume={18 4}, pages={1502-6} }