|
|||||
|
|
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors |
|
| Authors: | Vaisburg Arkadii Paquin Isabelle Bernstein Naomy Frechette Sylvie Gaudette Frederic Leit Silvana Moradei Oscar Raeppel Stephane Zhou Nancy Bouchain Giliane Woo Soon Hyung Jin Zhiyun Gillespie Jeff Wang James Fournel Marielle Yan Pu Theresa Trachy-Bourget Marie-Claude Robert Marie-France Lu Aihua Yuk Jimmy Rahil Jubrail Macleod A Robert Besterman Jeffrey M Li Zuomei Delorme Daniel |
| Affiliation: | aMethylGene Inc., Department of Chemistry, 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1 bMethylGene Inc., Department of Biology, 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1 cAuspex Pharmaceuticals, 1261 Liberty Way, Vista, CA 92081-8356, USA dNeurochem, 275 Armand-Frappier Blvd., Laval, Que., Canada H7V 4A7 eTakeda San Diego, 10410 Science Center Drive, San Diego, CA 92121, USA |
| Abstract: | 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. |
| Keywords: | Histone deacetylase inhibitors HDAC Benzamides Cancer cell proliferation |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |