ArticleMolecules (Basel, Switzerland)2025
Novel Azaborine-Based Inhibitors of Histone Deacetylases (HDACs).
Article in Molecules (Basel, Switzerland), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
2 citing papers in PubMed.
- Boron-Based Bioisosteres in Medicinal Chemistry: Advances in Heterocycles and Therapeutic.ChemMedChem · 2026Review
- Copper-Catalyzed Asymmetric Hydroboration of Alkynes to C-N Axially Chiral Azaborines via Dynamic Kinetic Resolution.Angewandte Chemie (International ed. in English) · 2026Article
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Authors and funding
5 authors.
Funding
Abstract
Aromatic ring systems appear ubiquitously in active pharmaceutical substances, such as FDA-approved histone deacetylase inhibitors. However, these rings reduce the water solubility of the molecules, which is a disadvantage during application. To address this problem, azaborine rings may be substituted for conventional aromatic ring systems. These are obtained by replacing two adjacent carbon atoms with boron and nitrogen. Incorporating B-N analogs in place of aromatic rings not only enhances structural diversity but also provides a strategy to navigate around patent-protected scaffolds. We synthesized azaborines, which are isosteric to naphthalene and indole, and utilized them as capping units for HDAC inhibitors. These molecules were attached to various aliphatic and aromatic linkers with different zinc-binding units, used in established active compounds. Nearly half of the twenty-four molecules tested exhibited inhibitory activity against at least one of the enzymes HDAC1, HDAC4, or HDAC8, with three compounds displaying IC
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