ArticleJournal of medicinal chemistry2010
Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 63 citations in OpenAlex.
- Article
- Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters · 2017Article
- Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.Bioorganic & medicinal chemistry · 2017Article
- Antibiotics in malaria therapy: which antibiotics except tetracyclines and macrolides may be used against malaria?Malaria journal · 2016Review
- Development of Novel Erythromycin Derivatives with Inhibitory Activity against Proliferation of Tumor Cells.PloS one · 2016Article
- A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.Bioorganic & medicinal chemistry · 2015Article
- Exploiting translational stalling peptides in an effort to extend azithromycin interaction within the prokaryotic ribosome nascent peptide exit tunnel.Bioorganic & medicinal chemistry · 2015Article
- Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects.Cancer research · 2014Article
- Macrolide-peptide conjugates as probes of the path of travel of the nascent peptides through the ribosome.ACS chemical biology · 2014Article
- The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.Bioorganic & medicinal chemistry letters · 2014Article
- Chemical metabolic inhibitors for the treatment of blood-borne cancers.Anti-cancer agents in medicinal chemistry · 2014Review
- Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.Journal of medicinal chemistry · 2013Article
- Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.Journal of medicinal chemistry · 2013Article
- Dual-acting histone deacetylase-topoisomerase I inhibitors.Bioorganic & medicinal chemistry letters · 2013Article
- 3-Hydroxypyridin-2-thione as novel zinc binding group for selective histone deacetylase inhibition.Journal of medicinal chemistry · 2013Article
- Molecular architecture of zinc chelating small molecules that inhibit spliceosome assembly at an early stage.RNA (New York, N.Y.) · 2012Article
- Targeted cancer therapy: giving histone deacetylase inhibitors all they need to succeed.Future medicinal chemistry · 2012Review
- Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.Journal of medicinal chemistry · 2012Article
- Structure, mechanism, and inhibition of histone deacetylases and related metalloenzymes.Current opinion in structural biology · 2011Review
- Macrocyclic histone deacetylase inhibitors.Current topics in medicinal chemistry · 2010Review
Corrections and comments
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Authors and funding
8 authors at 5 institutions in 1 country.
Funding
Abstract
Inhibition of histone deacetylase (HDAC) function is a validated therapeutic strategy for cancer treatment. Of the several structurally distinct small molecule histone deacetylase inhibitors (HDACi) reported, macrocyclic depsipeptides possess the most complex cap groups and have demonstrated excellent HDAC inhibition potency and isoform selectivity. Unfortunately, the development of macrocyclic depsipeptides has been hampered in part because of development problems characteristic of large peptides and the complex reaction schemes required for their synthesis. Herein we report that tricyclic ketolide TE-802 is an excellent mimetic for the peptide backbone of macrocyclic HDACi. Compounds derived from this template are particularly selective against HDACs 1 and 2 with nanomolar inhibitory activity. Interrogation of the association between a subset of these compounds and key HDAC isoforms, using AutoDock, enables a molecular description of the interaction between the HDAC enzyme's outer rim and the inhibitors' macrocyclic cap group that are responsible for compound affinity and presumably isoform selectivity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.