Drug intelligence / Profile preview

4-hydroxycoumarin

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Small Molecules
01

Overview

4-hydroxycoumarin is a small molecule and a hydroxy derivative of coumarin. It serves as the core scaffold for a class of anticoagulant drugs known as the 4-hydroxycoumarins (including warfarin and dicoumarol), which act as vitamin K antagonists by inhibiting vitamin K epoxide reductase. While derivatives with large aromatic substituents at the 3-position are potent anticoagulants used clinically to prevent and treat thromboembolic disorders, **the parent compound itself (4-hydroxycoumarin) is not an active anticoagulant** but is widely used in pharmaceutical research and synthesis. It also exhibits antioxidant properties and has been studied for potential antibacterial, antifungal, antiviral, anti-inflammatory, antitumor activities and as an inhibitor of HIV-1 integrase[1][2][3][5][6].

Other names
4-coumarinol4-hydroxy-2-chromenone4-hydroxy-2H-1-benzopyran-2-onebenzotetronic acidcoumarin, 4-hydroxy-4-OH coumarin
02

Targets

Integrase allosteric pocket (HIV)

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