Paper
Identification and optimisation of a series of substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Published Jan 15, 2007 · Steve Price, W. Bordogna, R. Bull
Bioorganic & medicinal chemistry letters
Q2 SJR score
37
Citations
1
Influential Citations
Abstract
Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.
In Vitro StudyStudy Snapshot
Substituted 5-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids show potent HDAC inhibitory activity and potential anti-proliferative activity, with compound 6j showing efficacy in a mouse xenograft experiment.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
Full text analysis coming soon...
References
Anticancer activities of histone deacetylase inhibitors
HDAC inhibitors show potential in reversing cancer-associated epigenetic changes, but their anticancer effects may be broader and more complex than initially understood.
2006·2860citations·Jessica E. Bolden et al.·Nature Reviews Drug Discovery
Nature Reviews Drug Discovery
Rational design of non-hydroxamate histone deacetylase inhibitors.
Non-hydroxamate HDAC inhibitors show promising inhibitory effects and antiproliferative activity, offering a promising alternative to hydroxamic acid derivatives for HDAC inhibitors.
2006·28citations·Takayoshi Suzuki et al.·Mini reviews in medicinal chemistry
Mini reviews in medicinal chemistry
Chromatin control and cancer-drug discovery: realizing the promise.
Recent advances in chromatin control research promise to lead to new, mechanism-based cancer treatments by modulating gene expression.
2006·71citations·A. Inche et al.·Drug discovery today
Drug discovery today
Histone deacetylase inhibitors: a survey of recent patents
Recent patenting activity in the field of HDAC inhibitors shows a continued interest by major pharmaceutical companies, with a few compounds progressing to human clinical trials.
2005·15citations·H. Weinmann et al.·Expert Opinion on Therapeutic Patents
Expert Opinion on Therapeutic Patents
Non-hydroxamate histone deacetylase inhibitors.
Non-hydroxamate HDAC inhibitors show potential as anticancer agents with few side effects and better selectivity among HDAC isozymes compared to hydroxamate inhibitors.
2005·106citations·Takayoshi Suzuki et al.·Current medicinal chemistry
Current medicinal chemistry
Citations
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Molecular hybrids show promise in cancer chemotherapy due to their ability to target multiple targets and diverse modes of action, offering potential for improved treatment outcomes.
2020·31citations·Shalini et al.·Expert Opinion on Drug Discovery
Expert Opinion on Drug Discovery
Computer-Aided Drug Design in Epigenetics
Computer-aided drug design has shown promise in speeding up epigenetic drug discovery, with methods like druggability prediction, virtual screening, and scaffold hopping successfully applied.
2018·58citations·Wenchao Lu et al.·Frontiers in Chemistry
Frontiers in Chemistry
Mechanistic Insights into the Binding of Class IIa HDAC Inhibitors toward Spinocerebellar Ataxia Type-2: A 3D-QSAR and Pharmacophore Modeling Approach
The 3D-QSAR model identified SEI and ACI as potential anti-ataxia compounds, with SEI showing higher inhibitory activity and ACI showing lower inhibitory activity.
2017·16citations·S. Sinha et al.·Frontiers in Neuroscience
Frontiers in Neuroscience
Inhibitors of histone deacetylase as antitumor agents: A critical review.
HDAC inhibitors show potential as anticancer agents by altering gene expression and regulating cell survival, differentiation, and apoptosis in tumor cells.
2016·188citations·M. Manal et al.·Bioorganic chemistry
Bioorganic chemistry
Virtual screening and experimental validation of novel histone deacetylase inhibitors
This study identified three new HDAC inhibitors, one of which shows anti-proliferative and apoptosis-inducing activity against various cancer cell lines, using a virtual screening workflow.
2016·25citations·Yan-xin Huang et al.·BMC Pharmacology & Toxicology
BMC Pharmacology & Toxicology
Fragment based G-QSAR and molecular dynamics based mechanistic simulations into hydroxamic-based HDAC inhibitors against spinocerebellar ataxia
Hydroxamic-based HDAC inhibitors HIC and DHC show potential as potent therapeutic leads against spinocerebellar ataxia type-2, with good binding and potential for structural substitutions to enhance inhibitory activity.
2016·28citations·S. Sinha et al.·Journal of Biomolecular Structure and Dynamics
Journal of Biomolecular Structure and Dynamics
NOVEL PYRAZOLINES: SYNTHESIS AND EVALUATION OF THEIR DERIVATIVES WITH ANTICANCER AND ANTI-INFLAMMATORY ACTIVITIES
Novel pyrazolines and chalcones synthesized show anticancer and anti-inflammatory properties, with methoxy-containing compounds showing anti-inflammatory activity.
2015·5citations·L. Reddy et al.·International Journal of Pharmacy and Pharmaceutical Sciences
International Journal of Pharmacy and Pharmaceutical Sciences
Comparative Modeling and Benchmarking Data Sets for Human Histone Deacetylases and Sirtuin Families
MUBD-HDACs are the most comprehensive and maximally unbiased benchmark data sets for HDACs, covering all classes and 14 isoforms, and can be applied unbiasedly to both ligand-based and SBVS approaches.
2015·25citations·J. Xia et al.·Journal of chemical information and modeling
Journal of chemical information and modeling