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


A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides were designed and synthesized. These compounds were shown to inhibit recombinant human HDAC1 with IC(50) 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 p21(WAF1/Cip1), and inhibited cellular proliferation. Certain compounds of this class also showed in vivo activity in various human tumor xenograft models in mice.

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@article{Vaisburg2007N2Aminophenyl4heteroarylmethylben, title={N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.}, author={Arkadii F Vaisburg and Isabelle Paquin and Naomy Bernstein and Sylvie Fr{\'e}chette and Fr{\'e}d{\'e}ric Gaudette and Silvana M Leit and Oscar M Moradei and St{\'e}phane L. Raeppel and Nancy Z Zhou and Giliane Bouchain and Soon Hyung Woo and Zhiyun Jin and Jeff Gillespie and James J. L. Wang and Marielle Fournel and Pu Theresa Yan and Marie-Claude Trachy-Bourget and Marie-France Robert and Aihua Lu and Jimmy Yuk and Jubrail Rahil and A Robert Macleod and Jeffrey M. Besterman and Zuomei Li and Daniel Delorme}, journal={Bioorganic & medicinal chemistry letters}, year={2007}, volume={17 24}, pages={6729-33} }