ReviewMolecules (Basel, Switzerland)2025
Coumarin Derivatives as Anticancer Agents: Mechanistic Landscape with an Emphasis on Breast Cancer.
Review in Molecules (Basel, Switzerland), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
10 citing papers in PubMed.
- Phthalazine as a medically versatile polyheterocyclic core with underexplored anticancer potential.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Artificial intelligence-driven discovery of coumarin-based therapeutics: Revolutionizing target identification and validation.Pharmaceutical science advances · 2026Review
- Coumarin derivatives as promising anticancer drugs: a comprehensive review from synthesis to anticancer applications.RSC advances · 2026Review
- Bergapten as a Multifunctional Phytochemical in Cancer Therapy: Mechanistic Insights, Pharmacokinetics, and Possible Nanotechnology-Enabled Formulation Strategies.Pharmaceutics · 2026Review
- Coumarins as modulators of autophagy and PI3K/mTOR signaling: implications for next-generation cancer therapies.Biomedical journal · 2026Review
- Identification of PI3K alpha inhibitors through large-scale virtual screening and integrated molecular modeling, biophysical characterization, and ADMET profiling.Scientific reports · 2026Article
- A Computational Investigation of Four Sesquiterpene [4+2] Trimers, Inubritantrimers A-D, and Their Synthetic Intermediates Isolated fromMolecules (Basel, Switzerland) · 2026Article
- Synthesis and Biological Evaluation of New Quinazolin-4(3H)-One-Coumarin Hybrids Designed as Anticancer and Antibacterial Agents.International journal of molecular sciences · 2026Article
- Coumarin-Amino Acid Hybrids Used as Possible Multifactorial Anti-Inflammatory Agents.International journal of molecular sciences · 2026Article
- Synthesis of some novel coumarin-based heterocycles, elucidation of their antifungal behavior, molecular docking and computational studies.Scientific reports · 2026Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Coumarin derivatives constitute a versatile small-molecule chemotype with broad anticancer potential. This narrative review synthesizes recent in vitro and in vivo evidence on coumarin-based scaffolds, emphasizing breast cancer and covering lung, prostate, and colorectal models. We summarize major mechanisms of action-including induction of apoptosis (caspase activation and BAX/BCL-2 balance), modulation of PI3K/Akt/mTOR signaling, inhibition of angiogenesis (VEGFR-2), interference with estrogen biosynthesis (aromatase/ER axis), chaperone targeting (Hsp90), and attenuation of multidrug resistance (efflux pumps/autophagy)-and highlight representative chemotypes (e.g., benzimidazole, triazole, furocoumarins, topoisomerase- and CDK-oriented hybrids). Where available, we contrast potency and selectivity across models (e.g., MCF-7 vs. MDA-MB-231; A549; PC-3; colon lines) and discuss structure-activity trends linking substituent patterns (heteroaryl linkers, judicious halogenation, polar handles) to pathway engagement. We also delineate translational gaps limiting clinical progress-selectivity versus non-malignant cells, incomplete pharmacokinetic and safety characterization, and limited validation beyond xenografts. Finally, we outline priorities for preclinical optimization: biology-aligned target selection with biomarkers, resistance-aware combinations (e.g., PI3K/mTOR ± autophagy modulation; MDR mitigation), and early integration of ADME/tox and PK/PD to confirm on-target exposure. Collectively, the evidence supports coumarins as adaptable, multi-target anticancer leads, particularly promising in hormone-dependent breast cancer while remaining relevant to other tumor types.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.