Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with
typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes
and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some
coumarin-based drugs such as anticoagulant and antineurodegenerative agents have been extensively used in clinic. Coumarin-containing
supramolecular medicinal agents as a new increasing expansion of supramolecular chemistry in pharmaceutical science have also been
actively investigated in recent years. Coumarin-derived artificial ion receptors, fluorescent probes and biological stains are growing
quickly and have a variety of potential applications in monitoring timely enzyme activity, complex biological events as well as accurate
pharmacological and pharmacokinetic properties. This review provides a systematic summary and insight of the whole range of medicinal
chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative,
antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive
agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains. Some rational design
strategies, structure-activity relationships and action mechanisms are discussed. The perspectives of the future development of coumarinbased
medicinal chemistry are also presented.
Antibacterial, anticancer, anticoagulant, antioxidative, biological stain, coumarin, probe, supramolecular drug.
Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715, People’s Republic of China.