Quinoxaline Derivatives in Anticancer and Antimicrobial Applications

Quinoxaline derivatives have emerged as a versatile class of N-heterocyclic compounds with dual functionality in oncology and anti-infective therapy. The rigid bicyclic framework of quinoxaline serves as a modifiable scaffold for installing substituents that enhance binding to diverse molecular targets. In anticancer research, tailored quinoxaline conjugates have been shown to inhibit kinases, disrupt microtubule dynamics and induce apoptosis selectively in tumour cells. Parallel efforts in antimicrobial applications exploit electron-rich substituents to interact with bacterial enzymes and fungal cell walls, yielding broad-spectrum activity against Gram-positive and Gram-negative pathogens. Structure–activity relationship studies guide the optimisation of lipophilicity, electronic distribution and hydrogen-bonding capacity to maximise potency while minimising toxicity to normal cells. Green synthetic routes and one-pot cascades have further advanced the accessibility of polysubstituted quinoxalines, underscoring the global relevance of this scaffold for drug discovery and public health.

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Quinoxaline Derivatives in Anticancer and Antimicrobial Applications publication trend

The graph below shows the total number of articles in quinoxaline derivatives in anticancer and antimicrobial applications across all publications each year (not limited to Nature Index journals).

Technical terms

Quinoxaline scaffold: A fused bicyclic ring system composed of a benzene ring fused to a pyrazine, serving as a core for chemical modification.

Structure–activity relationship (SAR): Analysis of how changes in molecular structure affect biological activity, guiding optimisation of efficacy and selectivity.

Cytotoxicity: The ability of a compound to kill or inhibit the growth of cells, often measured in cancer cell lines.

EC₅₀: The effective concentration of a compound that produces 50 % of its maximum response in a biological assay.

Minimum inhibitory concentration (MIC): The lowest concentration of an antimicrobial agent that prevents visible growth of a microorganism.

Apoptosis: Programmed cell death characterised by DNA fragmentation, membrane blebbing and caspase activation, often targeted in cancer therapy.

References

1. [1,2,4]triazolo[4,3-a]quinoxaline as Novel Scaffold in the Imiqualines Family: Candidates with Cytotoxic Activities on Melanoma Cell Lines. Molecules (2023).
2. Design, Synthesis and Cytotoxic Evaluation of Novel Chalcone Derivatives Bearing Triazolo[4,3-a]-quinoxaline Moieties as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects. Molecules (2017).
3. Design and Synthesis of New Quinoxaline Derivatives as Anticancer Agents and Apoptotic Inducers. Molecules (2019).
4. Novel Synthetic Routes to Prepare Biologically Active Quinoxalines and Their Derivatives: A Synthetic Review for the Last Two Decades. Molecules (2021).