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Review
. 2024 Sep;44(5):2035-2077.
doi: 10.1002/med.22032. Epub 2024 Mar 26.

Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA-approved drugs and clinical candidates

Venu Sharma  1 , Ankita Sharma  1   2 , Bhagyashri N Wadje  3 , Sandip B Bharate  1   2   3
Affiliations
Review

Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA-approved drugs and clinical candidates

Venu Sharma et al. Med Res Rev. 2024 Sep.

Abstract

Natural products have always served as an important source of drugs for treating various diseases. Among various privileged natural product scaffolds, the benzopyrone class of compounds has a substantial presence among biologically active compounds. One of the pioneering anticoagulant drugs, warfarin approved in 1954 bears a benzo-α-pyrone (coumarin) nucleus. The widely investigated psoriasis drugs, methoxsalen, and trioxsalen, also contain a benzo-α-pyrone nucleus. Benzo-γ-pyrone (chromone) containing drugs, cromoglic acid, and pranlukast were approved as treatments for asthma in 1982 and 2007, respectively. Numerous other small molecules with a benzopyrone core are under clinical investigation. The present review discusses the discovery, absorption, distribution, metabolism, excretion properties, and synthetic approaches for the Food and Drug Administration-approved and clinical-stage benzopyrone class of compounds. The role of the pyrone core in biological activity has also been discussed. The present review unravels the potential of benzopyrone core in medicinal chemistry and drug development.

Keywords: FDA; anticoagulant; benzopyrones; chromones; clinical trials; coumarins; psoralen.

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References

REFERENCES

    1. Vogel A. Darstellung von Benzoesäure aus der Tonka‐Bohne und aus den Meliloten—oder Steinklee—Blumen. Ann Phys. 1820;64(2):161‐166.
    1. Murray RD. The naturally occurring coumarins. In: Herz W, Falk H, Kirby GW, Moore RE, eds. Fortschritte der Chemie organischer Naturstoffe/Progress in the Chemistry of Organic Natural Products. Vol 83. Springer; 2002:1‐619.
    1. Lončarić M, Gašo‐Sokač D, Jokić S, Molnar M. Recent advances in the synthesis of Coumarin derivatives from different starting materials. Biomolecules. 2020;10(1):151.
    1. Carneiro A, Matos MJ, Uriarte E, Santana L. Trending topics on Coumarin and its derivatives in 2020. Molecules. 2021;26:501.
    1. Lacy A, O'Kennedy R. Studies on coumarins and coumarin‐related compounds to determine their therapeutic role in the treatment of cancer. Curr Pharm Des. 2004;10(30):3797‐3811.

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