2. Academic Validation
  3. (2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors

(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors

  • Bioorg Med Chem Lett. 2004 Jan 5;14(1):283-7. doi: 10.1016/j.bmcl.2003.08.083.
Arkadii Vaisburg 1,  Naomy Bernstein,  Sylvie Frechette,  Martin Allan,  Elie Abou-Khalil,  Silvana Leit,  Oscar Moradei,  Giliane Bouchain,  James Wang,  Soon Hyung Woo,  Marielle Fournel,  Pu T Yan,  Marie-Claude Trachy-Bourget,  Ann Kalita,  Carole Beaulieu,  Zuomei Li,  A Robert MacLeod,  Jeffrey M Besterman,  Daniel Delorme
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montreal, Quebec, Canada H4S 2A1. vaisburga@methylgene.com
PMID: 14684344 DOI: 10.1016/j.bmcl.2003.08.083
Abstract

A variety of omega-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC(50) values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAF1/Cip1 and caused cell-cycle arrest in human Cancer cells. Compounds in this class showed efficacy in human tumor xenograft models.

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