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BODIPY and aza-BODIPY Dyes for Theragnostic Applications
Sandra M Rojas-Montoya1, Mario E Cuevas-Galindo1, Mónica Farfán-Paredes2
1Facultad de Química, Departamento de Química Orgánica, Universidad Nacional Autónoma de México, Ciudad Universitaria, Ciudad de México, Mexico.
Handbook of Experimental Pharmacology
|August 5, 2026
Summary
BODIPY and aza-BODIPY fluorophores are versatile tools in theragnostic research, enabling advanced fluorescence imaging and therapies. Molecular engineering optimizes their optical properties for next-generation diagnostic and therapeutic agents.
Area of Science:
- Organic Chemistry
- Materials Science
- Biomedical Engineering
Background:
- BODIPY and aza-BODIPY fluorophores possess excellent photophysical properties, photostability, and structural versatility.
- Their ease of chemical functionalization allows diverse applications in theranostics.
Purpose of the Study:
- To review recent advances in the molecular engineering of BODIPY and aza-BODIPY systems for theranostic applications.
- To emphasize structural strategies for modulating optical properties and therapeutic performance.
Main Methods:
- Review of molecular engineering strategies for BODIPY and aza-BODIPY based systems.
- Analysis of structure-property relationships for optical and therapeutic modulation.
- Focus on activatable probes, photosensitizers, responsive sensors, and nanoplatforms.
Main Results:
- Rational molecular design has significantly expanded the biomedical potential of these fluorophores.
- Development of activatable probes, photosensitizers, and responsive molecular sensors.
- Creation of nanostructured theragnostic platforms for integrated diagnosis and treatment.
Conclusions:
- BODIPY and aza-BODIPY fluorophores are highly promising for developing advanced fluorescent theranostic agents.
- Continued molecular engineering efforts are crucial for realizing their full potential in medicine.
- Future opportunities lie in creating sophisticated, next-generation theranostic tools.

