Literature DB >> 12419380

Trifluoromethyl ketones as inhibitors of histone deacetylase.

Robin R Frey1, Carol K Wada, Robert B Garland, Michael L Curtin, Michael R Michaelides, Junling Li, Lori J Pease, Keith B Glaser, Patrick A Marcotte, Jennifer J Bouska, Shannon S Murphy, Steven K Davidsen.   

Abstract

Trifluoromethyl ketones were found to be inhibitors of histone deacetylases (HDACs). Optimization of this series led to the identification of submicromolar inhibitors such as 20 that demonstrated antiproliferative effects against the HT1080 and MDA 435 cell lines.

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Year:  2002        PMID： 12419380     DOI： 10.1016/s0960-894x(02)00754-0

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


  19 in total

Review 1.  Epigenetic mechanisms of regulation of Foxp3 expression.

Authors:  Girdhari Lal; Jonathan S Bromberg
Journal:  Blood       Date:  2009-07-29       Impact factor: 22.113

2.  Discovery of a new class of histone deacetylase inhibitors with a novel zinc binding group.

Authors:  Youxuan Li; Patrick M Woster
Journal:  Medchemcomm       Date:  2015-04-01       Impact factor: 3.597

3.  3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.

Authors:  Vishal Patil; Quaovi H Sodji; James R Kornacki; Milan Mrksich; Adegboyega K Oyelere
Journal:  J Med Chem       Date:  2013-04-18       Impact factor: 7.446

4.  Synthesis of a new trifluoromethylketone analogue of l-arginine and contrasting inhibitory activity against human arginase I and histone deacetylase 8.

Authors:  Monica Ilies; Daniel P Dowling; Patrick M Lombardi; David W Christianson
Journal:  Bioorg Med Chem Lett       Date:  2011-08-03       Impact factor: 2.823

5.  Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain.

Authors:  Changning Wang; Thomas E Eessalu; Vanessa N Barth; Charles H Mitch; Florence F Wagner; Yijia Hong; Ramesh Neelamegam; Frederick A Schroeder; Edward B Holson; Stephen J Haggarty; Jacob M Hooker
Journal:  Am J Nucl Med Mol Imaging       Date:  2013-12-15

6.  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

7.  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

8.  Investigating the selectivity of metalloenzyme inhibitors.

Authors:  Joshua A Day; Seth M Cohen
Journal:  J Med Chem       Date:  2013-10-14       Impact factor: 7.446

9.  Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.

Authors:  Aditya Sudheer Vaidya; Raghupathi Neelarapu; Antonett Madriaga; He Bai; Emma Mendonca; Hazem Abdelkarim; Richard B van Breemen; Sylvie Y Blond; Pavel A Petukhov
Journal:  Bioorg Med Chem Lett       Date:  2012-09-07       Impact factor: 2.823

10.  Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition.

Authors:  Yves Depetter; Silke Geurs; Flore Vanden Bussche; Rob De Vreese; Jorick Franceus; Tom Desmet; Olivier De Wever; Matthias D'hooghe
Journal:  Medchemcomm       Date:  2018-05-18       Impact factor: 3.597
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