Related Experiment Video
Updated: Oct 25, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
Strategic Development of Activatable Turn-On Fluorogenic Prodrugs of Celecoxib with Selective Anticancer Activity and
Roopjyoti Misra1, Pallavi Barman1, Dorothy Das2
1Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati, Assam781039, India.
Abstract:
Herein, we report the first examples of ROS-responsive fluorogenic prodrugs that enable sustained intracellular delivery of celecoxib with a fluorescence turn-on readout and exhibit selective anticancer activity with reduced cardiotoxicity. Spectroscopic and HPLC analysis confirmed efficient ROS-mediated activation and time-dependent release of both celecoxib and the fluorophore, providing mechanistic insights into the stimuli-triggered prodrug activation and the self-immolative drug release profile under physiological conditions. The lead prodrug Cou-Coxib exhibited selective anticancer activity in triple-negative breast cancer (MDA-MB-231) cells over non-malignant cells and showed excellent therapeutic efficacy by S phase arrest. Furthermore, Cou-Coxib ameliorated celecoxib-induced cardiotoxicity in H9C2 cardiomyoblasts. The fluorogenic drug delivery process was validated with turn-on fluorescence readout in aqueous and cellular media and subsequently in developing zebrafish embryos. Overall, this study underscores the rational design of fluorogenic prodrugs of celecoxib exhibiting selective anticancer activity in breast cancer with attenuated cardiotoxicity, thereby offering improved therapeutic potential.
More Related Videos
07:40A Data Integration Workflow to Identify Drug Combinations Targeting Synthetic Lethal Interactions
Published on: May 27, 2021
09:29Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
Published on: September 30, 2016
Related Concept Videos
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Prodrugs
Prodrugs help overcome...