Potent histone deacetylase inhibitors derived from 4-(aminomethyl)-N-hydroxybenzamide with high selectivity for the HDAC6 isoform.

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2013-09-04

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/jm400385rPMID 23964961
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Results from a pivotal, open-label, phase II study of romidepsin in relapsed or refractory peripheral T-cell lymphoma after prior systemic therapy.

  2012cited by this paper
• Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A.

  2010cited by this paper
• Computational studies on the histone deacetylases and the design of selective histone deacetylase inhibitors.

  2009cited by this paper
• Inhibition of HDAC6‐dependent carcinogenesis: Emerging, new therapeutic options besides belinostat

  2009cited by this paper
• Human HDAC7 Harbors a Class IIa Histone Deacetylase-specific Zinc Binding Motif and Cryptic Deacetylase Activity*

  2008cited by this paper
• Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase.

  2008cited by this paper
• Solvent-free microwave synthesis of 3-(4-benzo〔b〕-thiophene-2-carbonyl)-1-piperazinyl-1-benzo〔b〕thiophen-2-yl-1-propanones: new hetero bis-ligands with potential 5-HT1A serotonergic activity

  2008cited by this paper
• Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.

  2008cited by this paper
• Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain*

  2008cited by this paper
• HDAC6 a new cellular stress surveillance factor

  2008cited by this paper
• The cytoplasmic deacetylase HDAC6 is required for efficient oncogenic tumorigenesis.

  2008cited by this paper
• The aggresome pathway as a target for therapy in hematologic malignancies.

  2008cited by this paper
• The ubiquitin-like modifier FAT10 interacts with HDAC6 and localizes to aggresomes under proteasome inhibition

  2008cited by this paper
• Histone deacetylase inhibitors: from bench to clinic.

  2008cited by this paper
• Chemistry, Biology, and QSAR Studies of Substituted Biaryl Hydroxamates and Mercaptoacetamides as HDAC Inhibitors—Nanomolar‐Potency Inhibitors of Pancreatic Cancer Cell Growth

  2008cited by this paper
• Role of the aggresome pathway in cancer: targeting histone deacetylase 6-dependent protein degradation.

  2008cited by this paper
• Structural origin of selectivity in class II-selective histone deacetylase inhibitors.

  2008cited by this paper
• HDAC6 rescues neurodegeneration and provides an essential link between autophagy and the UPS

  2007cited by this paper
• Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.

  2007cited by this paper
• HDAC6, at the crossroads between cytoskeleton and cell signaling by acetylation and ubiquitination

  2007cited by this paper
• 2-aroylindoles and 2-aroylbenzofurans with N-hydroxyacrylamide substructures as a novel series of rationally designed histone deacetylase inhibitors.

  2007cited by this paper
• Linking of autophagy to ubiquitin-proteasome system is important for the regulation of endoplasmic reticulum stress and cell viability.

  2007cited by this paper
• Zinc binding in HDAC inhibitors: a DFT study.

  2007cited by this paper
• Structure-activity relationship of 6-methylidene penems bearing 6,5 bicyclic heterocycles as broad-spectrum beta-lactamase inhibitors: evidence for 1,4-thiazepine intermediates with C7 R stereochemistry by computational methods.

  2006cited by this paper
• Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer

  2006cited by this paper
• HDAC6 and Microtubules Are Required for Autophagic Degradation of Aggregated Huntingtin*

  2005cited by this paper
• Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.

  2005cited by this paper
• Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma.

  2005cited by this paper
• Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases.

  2004cited by this paper
• Crystal structure of a eukaryotic zinc-dependent histone deacetylase, human HDAC8, complexed with a hydroxamic acid inhibitor.

  2004cited by this paper
• Histone deacetylase inhibitors.

  2004cited by this paper
• Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis.

  2004cited by this paper
• A fluorogenic histone deacetylase assay well suited for high-throughput activity screening.

  2003cited by this paper
• Structural biasing elements for in-cell histone deacetylase paralog selectivity.

  2003cited by this paper
• The deacetylase HDAC6 regulates aggresome formation and cell viability in response to misfolded protein stress.

  2003cited by this paper
• Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation

  2003cited by this paper

• A new computational cross-structure-activity relationship (C-SAR) approach applies to a selective HDAC6 inhibitor dataset for accelerated structure development

  2025cites this paper
• Challenging triple negative breast cancer through HDAC6 selective inhibition: Novel cap-group identification, structure-activity relationships, computational and biological studies.

  2025cites this paper
• Design, synthesis, and biological evaluation of tetrahydroisoquinoline based hydroxamate derivatives as HDAC 6 inhibitors for cancer therapy

  2023cites this paper
• Virtual screening for early identification of potent and selective histone deacetylase 6 inhibitor series.

  2023cites this paper
• Efficacy of selective histone deacetylase 6 inhibition in mouse models of Pseudomonas aeruginosa infection: A new glimpse for reducing inflammation and infection in cystic fibrosis.

  2022cites this paper
• HDAC6: A unique HDAC family member as a cancer target

  2022cites this paper
• Do biological activities of selective histone deacetylase 6 (HDAC6) inhibitors rely on the modification of cap group?

  2022cites this paper
• 1,2,3,4-Tetrahydroisoquinoline (THIQ) as privileged scaffold for anticancer de novo drug design

  2021cites this paper
• Strategies To Design Selective Histone Deacetylase Inhibitors

  2021cites this paper
• A carrier-free nanoparticle with dual NIR/acid responsiveness by co-assembly of enediyne and IR820 for combined PTT/chemotherapy.

  2021cites this paper
• Recent Progress in Histone Deacetylase Inhibitors as Anticancer Agents.

  2020cites this paper
• Recent advances in small molecular modulators targeting histone deacetylase 6

  2020cites this paper
• Design, Synthesis and Evaluation of Novel Indirubin-based N-Hydroxybenzamides, N-Hydroxypropenamides and N-Hydroxyheptanamides as Histone Deacetylase Inhibitors and Antitumor Agents.

  2020cites this paper
• HDAC6—An Emerging Target Against Chronic Myeloid Leukemia?

  2020cites this paper
• Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.

  2019cites this paper
• Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 (HDAC6) Inhibitors

  2019cites this paper
• Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.

  2019cites this paper
• Next-generation of selective histone deacetylase inhibitors

  2019cites this paper
• How Does Chirality Determine the Selective Inhibition of Histone Deacetylase 6? A Lesson from Trichostatin A Enantiomers Based on Molecular Dynamics.

  2019cites this paper
• Design, synthesis and evaluation of novel N-hydroxybenzamides/N-hydroxypropenamides incorporating quinazolin-4(3H)-ones as histone deacetylase inhibitors and antitumor agents.

  2018cites this paper
• HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.

  2018cites this paper
• 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.

  2018cites this paper
• Recent advances in the discovery of potent and selective HDAC6 inhibitors.

  2018cites this paper
• Development of a UV-Cleavable Protecting Group for Hydroxylamines, Synthesis of a StructurallyWide Variety of Hydroxamic Acids, and Identification of Histone Deacetylase Inhibitors

  2017cites this paper
• The Search for Potent, Small‐Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat

  2017cites this paper
• Synthesis and applications of benzohydroxamic acid-based histone deacetylase inhibitors.

  2017cites this paper
• Medicinal Chemistry Insights into Novel HDAC Inhibitors: An Updated Patent Review (2012-2016).

  2017cites this paper
• Anti-cancer effects of naturally derived compounds targeting histone deacetylase 6-related pathways.

  2017cites this paper
• Inside HDACs with more selective HDAC inhibitors.

  2016cites this paper
• Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.

  2016cites this paper
• Exploration of Novel Inhibitors for Class I Histone Deacetylase Isoforms by QSAR Modeling and Molecular Dynamics Simulation Assays

  2015cites this paper
• Discovery of a Novel HDAC2 Inhibitor by a Scaffold-Merging Hybrid Query.

  2015cites this paper
• Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.

  2015cites this paper
• [Histone deacetylase 6: structure, functions and development of selective inhibitors].

  2015cites this paper
• HDAC 6 Inhibitors Modulate Lys 49 Acetylation and Membrane Localization of β-Catenin in Human iPSC-Derived Neuronal Cells

  2015cites this paper
• Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors.

  2015cites this paper
• Histone deacetylase 6 in health and disease.

  2015cites this paper
• Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next

  2014cites this paper
• Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.

  2014cites this paper
• Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.

  2014cites this paper
• HDAC6 Inhibitors Modulate Lys49 Acetylation and Membrane Localization of β-Catenin in Human iPSC-Derived Neuronal Cells

  2014cites this paper
• Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.

  2014cites this paper
• Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors.

  2014cites this paper