{
  "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.",
  "abstract_shown": true,
  "affiliations": [
    "Department of Chemistry, Covenant University Km 10, Idiroko Road Ota Nigeria ola.ajani@covenantuniversity.edu.ng +234-8061670254.",
    "Covenant University Bioinformatics Research (CUBRe) Cluster Km 10, Idiroko Road Ota Nigeria.",
    "West African Centre for Cell Biology of Infectious Pathogens (WACCBIP), College of Basic and Applied Sciences, University of Ghana Legon-Accra Ghana.",
    "Holistic Drug Discovery and Development (H3D) Centre, Department of Chemistry, University of Cape Town Rondebosch 7701 South Africa."
  ],
  "article_type": "review article",
  "arxiv": null,
  "author_total": 5,
  "authors": [
    {
      "affs": [
        0,
        1
      ],
      "name": "Olayinka O Ajani",
      "orcid": "0000-0002-3422-3478"
    },
    {
      "affs": [
        0,
        2
      ],
      "name": "Gbolahan O Oduselu",
      "orcid": "0000-0003-0136-1732"
    },
    {
      "affs": [
        0
      ],
      "name": "Edidiong S Sam",
      "orcid": "0009-0009-8064-0553"
    },
    {
      "affs": [
        0
      ],
      "name": "Mfonobong L Ekpene"
    },
    {
      "affs": [
        3
      ],
      "name": "Oluwatosin Y Audu"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/darww81t8f2qv.bib",
  "cited_by": 0,
  "doi": "10.1039/d6ra03929d",
  "fulltext_url": "https://europepmc.org/articles/PMC13715860",
  "id": "darww81t8f2qv",
  "issns": [
    "2046-2069"
  ],
  "landing_url": "https://europepmc.org/article/MED/42953455",
  "language": "eng",
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "heading",
      "Chemistry"
    ],
    [
      "openalex",
      "1605|Synthesis and biological activity"
    ]
  ],
  "openalex": "W7224124751",
  "pdf_url": "https://europepmc.org/articles/PMC13715860?pdf=render",
  "pmcid": "PMC13715860",
  "pmid": "42953455",
  "published": "2026-10-28",
  "publisher": "Royal Society of Chemistry",
  "ris": "https://research.draconitic.com/paper/darww81t8f2qv.ris",
  "sources": [
    {
      "first_seen": "2026-10-31T00:20:40Z",
      "native_id": "MED:42953455",
      "source": "europepmc",
      "url": "https://europepmc.org/article/MED/42953455"
    },
    {
      "first_seen": "2026-11-01T12:23:03Z",
      "native_id": "PMC13715860",
      "source": "pmc",
      "url": "https://doi.org/10.1039/d6ra03929d"
    }
  ],
  "subjects": [
    {
      "field": "chemistry",
      "origin": "openalex:1605|Synthesis and biological activity",
      "subfield": "organic"
    }
  ],
  "title": "Recent advancements in the chemistry and therapeutic potential of coumarin motifs.",
  "title_text": "Recent advancements in the chemistry and therapeutic potential of coumarin motifs.",
  "type": "peer-reviewed",
  "updated_at": "2026-11-01T12:23:03Z",
  "url": "https://research.draconitic.com/paper/darww81t8f2qv",
  "venue": "RSC advances",
  "versions": []
}