A twenty-year journey exploring coumarin-based derivatives as bioactive molecules

Area of Science:

• Medicinal Chemistry
• Organic Chemistry
• Pharmacology

Background:

• The coumarin core (1-benzopyran-2(2H)-one) is a prevalent structural motif in natural products and bioactive molecules.
• Coumarin derivatives exhibit a wide spectrum of pharmacological activities, including anticoagulant, anti-inflammatory, antimicrobial, anti-HIV, and antitumor effects.

Purpose of the Study:

• To present a comprehensive overview of 20 years of research on the coumarin core.
• To highlight the utilization of the coumarin scaffold and pharmacophore in the design of novel biologically active small molecules by Prof. Angelo Carotti's research group.

Main Methods:

• Literature review and synthesis of scientific results.
• Exploitation of the coumarin core as a scaffold and pharmacophore in drug design.

Main Results:

• Detailed reporting of key scientific findings from two decades of coumarin research.
• Demonstration of the versatility of coumarin derivatives in yielding diverse biological activities.

Conclusions:

• The coumarin core is a valuable and versatile scaffold for the development of novel therapeutic agents.
• Continued investigation into coumarin derivatives holds significant promise for discovering new drugs with various pharmacological applications.