Recent advancements in the chemistry and therapeutic potential of coumarin motifs.
4 affiliations
- 1Department of Chemistry, Covenant University Km 10, Idiroko Road Ota Nigeria [email protected] +234-8061670254.
- 2Covenant University Bioinformatics Research (CUBRe) Cluster Km 10, Idiroko Road Ota Nigeria.
- 3West African Centre for Cell Biology of Infectious Pathogens (WACCBIP), College of Basic and Applied Sciences, University of Ghana Legon-Accra Ghana.
- 4Holistic Drug Discovery and Development (H3D) Centre, Department of Chemistry, University of Cape Town Rondebosch 7701 South Africa.
Abstract
Coumarin is an oxygen-containing heterocyclic scaffold of considerable importance in medicinal chemistry because of its structural versatility, natural occurrence, and broad range of pharmacological activities. This review provides an integrated overview of the historical development, natural occurrence, physical and chemical properties, synthetic approaches, pharmacological activities, biological targets, structure-activity relationships (SAR), and available toxicological information of coumarin derivatives. Recent literature on coumarin synthesis is examined, with emphasis on Pechmann, Perkin, Knoevenagel, microwave-assisted, metal-catalyzed, and contemporary functionalization strategies. The review also highlights representative clinically established coumarin-based compounds and investigational derivatives, together with their quantitative biological activities, mechanisms of action, and relevant structural features. Reported pharmacological activities include anticoagulant, antimicrobial, antimalarial, antileishmanial, antiviral, antifungal, antioxidant, antidiabetic, antidepressant, anticancer, anti-inflammatory, analgesic, and enzyme-inhibitory activities. Particular attention is given to recurring SAR patterns and biological targets that may guide the rational modification of the coumarin scaffold. Available toxicological and safety data are also considered, highlighting the importance of balancing pharmacological efficacy with therapeutic safety. In addition, the review identifies limitations in the current evidence, including fragmented SAR information, limited mechanistic and in vivo validation, and insufficient toxicity data for several investigational derivatives. By integrating synthetic chemistry with pharmacological, mechanistic, SAR, and safety considerations, this review provides a comprehensive perspective on the current progress of coumarin research and highlights opportunities for the development of coumarin-based small-molecule therapeutics.
Related
- A Mini-Review on Thalidomide: Chemistry, Mechanisms of Action, Therapeutic Potential and Anti-Angiogenic Properties in Multiple Myeloma
- Recent Advancements in Polymer and Graphene-Based Composites for High-Performance Supercapacitor Applications: Progress, Challenges, and Future Perspectives
- In silico investigation of fenugreek-derived coumarin and its potential impact on human health
- New thiazole/coumarin hybrids as EGFR inhibitors with potential VEGFR-2 inhibition (design, synthesis, biological evaluation, and dynamic stimulation).
- Recent Advances in Polysaccharides from Sophora flavescens Ait.: Extraction, Purification, Structural Characteristics, Pharmacological Effects, Structure-Activity Relationships, and Potential Applications
BibTeX
@article{ajani2026recent,
title = {{Recent advancements in the chemistry and therapeutic potential of coumarin motifs.}},
author = {Olayinka O Ajani and Gbolahan O Oduselu and Edidiong S Sam and Mfonobong L Ekpene and Oluwatosin Y Audu},
journal = {RSC advances},
year = {2026},
month = oct,
doi = {10.1039/d6ra03929d},
url = {https://europepmc.org/article/MED/42953455},
note = {CC BY},
}
RIS
TY - JOUR
TI - Recent advancements in the chemistry and therapeutic potential of coumarin motifs.
AU - Olayinka O Ajani
AU - Gbolahan O Oduselu
AU - Edidiong S Sam
AU - Mfonobong L Ekpene
AU - Oluwatosin Y Audu
PY - 2026
DA - 2026/10/28
JO - RSC advances
DO - 10.1039/d6ra03929d
UR - https://europepmc.org/article/MED/42953455
AB - Coumarin is an oxygen-containing heterocyclic scaffold of considerable importance in medicinal chemistry because of its structural versatility, natural occurrence, and broad range of pharmacological activities. This review provides an integrated overview of the historical development, natural occurrence, physical and chemical properties, synthetic approaches, pharmacological activities, biological targets, structure-activity relationships (SAR), and available toxicological information of coumarin derivatives. Recent literature on coumarin synthesis is examined, with emphasis on Pechmann, Perkin, Knoevenagel, microwave-assisted, metal-catalyzed, and contemporary functionalization strategies. The review also highlights representative clinically established coumarin-based compounds and investigational derivatives, together with their quantitative biological activities, mechanisms of action, and relevant structural features. Reported pharmacological activities include anticoagulant, antimicrobial, antimalarial, antileishmanial, antiviral, antifungal, antioxidant, antidiabetic, antidepressant, anticancer, anti-inflammatory, analgesic, and enzyme-inhibitory activities. Particular attention is given to recurring SAR patterns and biological targets that may guide the rational modification of the coumarin scaffold. Available toxicological and safety data are also considered, highlighting the importance of balancing pharmacological efficacy with therapeutic safety. In addition, the review identifies limitations in the current evidence, including fragmented SAR information, limited mechanistic and in vivo validation, and insufficient toxicity data for several investigational derivatives. By integrating synthetic chemistry with pharmacological, mechanistic, SAR, and safety considerations, this review provides a comprehensive perspective on the current progress of coumarin research and highlights opportunities for the development of coumarin-based small-molecule therapeutics.
SN - 2046-2069
ER -