Related Experiment Video

Updated: Dec 22, 2025

Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts

Published on: June 26, 2018

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Recent Developments of Target Based Coumarin Derivatives as Potential Anticancer Agents

Nerella Sridhar Goud1, Pardeep Kumar1, Rose Dawn Bharath1

  • 1Department of Neuroimaging and Interventional Radiology (NI & IR), National Institute of Mental Health and Neuro Sciences (NIMHANS), Bengaluru-560 029, India.

Mini Reviews in Medicinal Chemistry
|May 11, 2020
PubMed

Insights

Coumarin derivatives show promise as novel anticancer drugs, offering diverse mechanisms to combat multidrug-resistant cancers. This review explores target-based coumarin compounds and their synthesis for improved cancer therapy.

Area of Science:

  • Medicinal Chemistry
  • Organic Chemistry
  • Pharmacology

Background:

  • Cancer is a leading global cause of death, with 9.6 million deaths in 2018.
  • Multidrug resistance and lack of selectivity in current cancer treatments necessitate novel therapeutic agents.
  • Coumarin scaffolds are widely utilized for developing effective anticancer drugs due to their versatile mechanisms.

Purpose of the Study:

  • To review target-based coumarin derivatives for cancer therapy.
  • To highlight diverse mechanisms of action for coumarin-based anticancer agents.
  • To discuss synthetic strategies for developing coumarin derivatives.

Main Methods:

  • Literature review of coumarin derivatives targeting cancer.
  • Analysis of Structure-Activity Relationships (SAR) for coumarin compounds.
  • Focus on coumarins targeting specific proteins like Galectin-1, Carbonic anhydrases, and Tubulin.

Main Results:

  • Coumarin derivatives exhibit potent anticancer activity through various mechanisms.
  • Target-based design, including Galectin-1, Carbonic anhydrases, and Tubulin inhibition, shows efficacy.
  • SAR studies guide the development of coumarins with enhanced potency and reduced side effects.

Conclusions:

  • Coumarin derivatives represent a promising class of anticancer agents.
  • Target-specific coumarin development offers a viable strategy for overcoming drug resistance.
  • Further research into synthetic strategies can accelerate the discovery of novel coumarin-based cancer therapeutics.
Keywords:
Coumarincancermultidrug-resistantspecific targetssynthetic strategiestubulin protein

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