Literature DB >> 12951120

Alpha-keto amides as inhibitors of histone deacetylase.

Carol K Wada1, Robin R Frey, Zhiqin Ji, Michael L Curtin, Robert B Garland, James H Holms, Junling Li, Lori J Pease, Jun Guo, Keith B Glaser, Patrick A Marcotte, Paul L Richardson, Shannon S Murphy, Jennifer J Bouska, Paul Tapang, Terrance J Magoc, Daniel H Albert, Steven K Davidsen, Michael R Michaelides.   

Abstract

Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.

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Year:  2003        PMID: 12951120     DOI: 10.1016/s0960-894x(03)00685-1

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


  5 in total

1.  Homology modeling, force field design, and free energy simulation studies to optimize the activities of histone deacetylase inhibitors.

Authors:  Hwangseo Park; Sangyoub Lee
Journal:  J Comput Aided Mol Des       Date:  2004-06       Impact factor: 3.686

2.  Complex structure of a bacterial class 2 histone deacetylase homologue with a trifluoromethylketone inhibitor.

Authors:  Tine Kragh Nielsen; Christian Hildmann; Daniel Riester; Dennis Wegener; Andreas Schwienhorst; Ralf Ficner
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2007-03-23

3.  Synthesis of alpha-keto-imides via oxidation of ynamides.

Authors:  Ziyad F Al-Rashid; Whitney L Johnson; Richard P Hsung; Yonggang Wei; Pei-Yuan Yao; Renhei Liu; Kang Zhao
Journal:  J Org Chem       Date:  2008-10-21       Impact factor: 4.354

4.  Convergent synthesis of alpha-ketoamide inhibitors of Pin1.

Authors:  Guoyan G Xu; Felicia A Etzkorn
Journal:  Org Lett       Date:  2010-02-19       Impact factor: 6.005

5.  Search for the pharmacophore of histone deacetylase inhibitors using pharmacophore query and docking study.

Authors:  Atefeh Haji Agha Bozorgi; Afshin Zarghi
Journal:  Iran J Pharm Res       Date:  2014       Impact factor: 1.696

  5 in total

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