Literature DB >> 14684344

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

Arkadii Vaisburg1, 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.   

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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Year:  2004        PMID: 14684344     DOI: 10.1016/j.bmcl.2003.08.083

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

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Journal:  Molecules       Date:  2022-06-16       Impact factor: 4.927

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3.  Structural Refinement of 2,4-Thiazolidinedione Derivatives as New Anticancer Agents Able to Modulate the BAG3 Protein.

Authors:  Dafne Ruggiero; Stefania Terracciano; Gianluigi Lauro; Michela Pecoraro; Silvia Franceschelli; Giuseppe Bifulco; Ines Bruno
Journal:  Molecules       Date:  2022-01-20       Impact factor: 4.411

4.  3-[(R)-1-Hy-droxy-butan-2-yl]-1,2,3-benzo-triazin-4(3H)-one.

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5.  Cytotoxicity evaluation of a new set of 2-aminobenzo[de]iso-quinoline-1,3-diones.

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Journal:  Int J Mol Sci       Date:  2014-12-04       Impact factor: 5.923

  5 in total

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