Chromenochalcones: a comprehensive review on developments towards a medicinal perspective

Area of Science:

• Medicinal Chemistry
• Natural Products Chemistry
• Drug Discovery

Background:

• Chalcones are versatile scaffolds in medicinal chemistry due to their reactive α,β-unsaturated carbonyl group.
• Pyranochalcones and chromanchalcones are subclasses of flavonoids with broad biological activities.
• The structural flexibility of chalcones allows for extensive modification and exploration in drug discovery.

Purpose of the Study:

• To provide a comprehensive review of the preclinical research on chromenochalcones and their derivatives.
• To highlight the significant therapeutic potential of chromenochalcones across various disease areas.
• To discuss synthetic pathways for pyranochalcones to aid future drug development.

Main Methods:

• Systematic investigation of scientific databases to compile relevant literature.
• Focus on preclinical data illustrating the biological functions of chromenochalcones.
• Inclusion of synthetic methodologies for selected pyranochalcones.

Main Results:

• Chromenochalcones demonstrate significant antimalarial, anti-inflammatory, antileishmanial, cytotoxic, antibacterial, antifungal, and antioxidant activities.
• Preclinical evidence supports the therapeutic potential of these compounds.
• Key synthetic routes for pyranochalcones like mallaophilippens C and E, citrunobin, and lesperol are presented.

Conclusions:

• Chromenochalcones represent a promising template for the development of novel therapeutic agents.
• The reviewed data provides a foundation for designing potent medications based on established synthetic strategies.
• Further research into chromenochalcones is warranted to translate their preclinical potential into clinical applications.