ArticleMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents2026
Exploring new quinoxaline, quinoline, and naphthalene carboxamides as HDAC-targeted anticancer agents: Cytotoxicity, enzymatic HDAC evaluation, and in silico studies.
Article in Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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Who cites it
1 citing paper in PubMed.
- 6-(2-Aminoethyl)-6Biomolecules · 2026Article
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10 authors.
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Abstract
Histone deacetylase inhibitors (HDACis) are important epigenetic anticancer agents, but new HDAC-targeted scaffolds are still needed to improve biological profiles. Herein, quinoxaline, quinoline, and naphthalene were selected as structurally related fused-aromatic cap groups within the HDAC inhibitor pharmacophore, allowing comparison of naphthalene and its aza-analogs in a unified carboxamide series. A new series of quinoxaline, quinoline, and naphthalene carboxamides was synthesized through amidation of amino acid methyl esters, followed by hydrolysis, hydrazinolysis, and hydroxamate formation. Their structures were confirmed by spectroscopic and mass spectrometric analyses. Cytotoxicity was evaluated against A549, HeLa, and MCF-7 cancer cells and non-cancerous Vero cells using the MTT assay. Most derivatives were weakly active; however, hydroxamic acids showed improved potency. Compound 10d exhibited submicromolar cytotoxicity against A549, HeLa, and MCF-7 cells (IC
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