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March 13, 2026PharmaceuticsOpen Access

Coumarin-Based Prodrugs: Therapeutic Promise or Still Confined to Preclinical Exploration?

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Authors

AAAtziri Corin Chavez AlvarezEMEmmanuel Moreau

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Overview

This review evaluates coumarin-based prodrugs' therapeutic potential in various diseases, highlighting translational challenges.

Key Points

  • The aim is to assess the therapeutic potential of coumarin-based prodrugs and their preclinical status.
  • Review of coumarin scaffolds in prodrug design
  • Evaluation of activation strategies including enzymatic, pH, redox, and light-triggered methods
  • Analysis of preclinical studies across oncology, inflammation, infectious diseases, and cardiovascular disorders
  • Coumarin-based prodrugs show improved bioavailability and reduced off-target toxicity in preclinical models.
  • Real-time fluorescence monitoring is achieved through some prodrug designs.
  • Most prodrugs remain at the in vitro or small-animal model stage, with limited clinical translation.

Cite This Study

Alvarez et al. (2026) studied this question.

synapsesocial.com/papers/69b3acc502a1e69014cceb3ehttps://doi.org/10.3390/pharmaceutics18030341
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Also Consider

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  1. 1Coumarin derivatives in pharmaceutical and biomedical engineering: Advances in design, synthesis, and therapeutic applications2025
  2. 2The Role of Coumarins in Drug Discovery: Pharmacological Insights andStructural Innovations2026 · 2 citations
  3. 3A COMPREHENSIVE REVIEW ON PHARMACOLOGICAL IMPORTANCE OF COUMARIN AND ITS DERIVATIVES2026
  4. 4Syntheses, reactivity, and biological applications of coumarins2024 · 63 citations
  5. 5Coumarin and Its Derivatives: Recent Advances in Synthetic Strategies and Biological Activities2026