ArticleACS medicinal chemistry letters2013
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Synthesis and Biological Evaluation of Colibactin Derivatives.ACS chemical biology · 2026Article
- Exploration of Fingerprints and Data Mining-based Prediction of Some Bioactive Compounds fromCurrent computer-aided drug design · 2025Article
- Progress in discovery and development of natural inhibitors of histone deacetylases (HDACs) as anti-cancer agents.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- HDAC9 as a Privileged Target: Reviewing its Role in Different Diseases and Structure-activity Relationships (SARs) of its Inhibitors.Mini reviews in medicinal chemistry · 2024Review
- Marine Power on Cancer: Drugs, Lead Compounds, and Mechanisms.Marine drugs · 2021Review
- Thiazole-amino acids: influence of thiazole ring on conformational properties of amino acid residues.Amino acids · 2021Article
- Process Development and Scale-up Total Synthesis of Largazole, a Potent Class I Histone Deacetylase Inhibitor.Organic process research & development · 2018Article
- Synthesis and biological evaluation of largazole zinc-binding group analogs.Bioorganic & medicinal chemistry · 2017Article
- Variable active site loop conformations accommodate the binding of macrocyclic largazole analogues to HDAC8.Biochemistry · 2015Article
- An overview of naturally occurring histone deacetylase inhibitors.Current topics in medicinal chemistry · 2015Review
- The application of click chemistry in the synthesis of agents with anticancer activity.Drug design, development and therapy · 2015Review
- Evaluation of class I HDAC isoform selectivity of largazole analogues.Bioorganic & medicinal chemistry letters · 2014Article
- Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.ACS medicinal chemistry letters · 2014Article
Corrections and comments
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Authors and funding
9 authors.
Funding
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Abstract
We report the design, synthesis, and biological evaluation of a new series of largazole analogues in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, respectively. Compound 7 bearing a tetrazole ring was identified to show much better selectivity for HDAC1 over HDAC9 than largazole (10-fold). This work could serve as a foundation for further exploration of selective HDAC inhibitors using a largazole molecular scaffold.
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