Coumarin Derivatives in Pharmacological Applications
Summary
Coumarin derivatives encompass a diverse class of benzopyrone-based heterocycles valued for their privileged scaffold in medicinal chemistry. These compounds occur naturally in numerous plants and can be readily synthesised, allowing extensive structural modification to enhance target specificity and pharmacokinetic properties. Their pharmacological repertoire spans anticancer, anti-inflammatory, antimicrobial, anticoagulant, neuroprotective and antioxidant activities. Mechanistic modes include enzyme inhibition, modulation of signal transduction pathways, free-radical scavenging, induction of cell-cycle arrest and apoptosis. Recent advances focus on the design of multitarget ligands to address complex diseases such as neurodegeneration and malignancy, optimisation of bioavailability and exploration of photochemotherapeutic applications. The global appeal of coumarins rests on their low toxicity, synthetic accessibility and translational potential from bench to clinical evaluation.
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Coumarin Derivatives in Pharmacological Applications publication trend
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Technical terms
Coumarin: A benzopyrone heterocycle forming the core structure of this class of compounds.
Scaffold: A core molecular framework used as a basis for systematic chemical modification in drug design.
Multitarget ligand: A compound engineered to engage multiple biological targets concurrently.
Structure–Activity Relationship: Analysis of how variations in chemical structure influence biological efficacy.
Keap1/Nrf2/ARE signalling pathway: A cellular defence mechanism that regulates expression of antioxidant and cytoprotective genes.
References
- Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds. Molecules (2018).
- An Overview of Coumarin as a Versatile and Readily Accessible Scaffold with Broad-Ranging Biological Activities. International Journal of Molecular Sciences (2020).
- Coumarins as Modulators of the Keap1/Nrf2/ARE Signaling Pathway. Oxidative Medicine and Cellular Longevity (2020).
- Natural Coumarins: Exploring the Pharmacological Complexity and Underlying Molecular Mechanisms. Oxidative Medicine and Cellular Longevity (2021).
- Recent advances on anticancer activity of coumarin derivatives. European Journal of Medicinal Chemistry Reports (2022).
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