Coumarin as an Elite Scaffold in Anti-Breast Cancer Drug Development: Design Strategies, Mechanistic Insights, and...

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Oncology

Background:

• Breast cancer is a leading cause of death in women, with current treatments facing resistance and toxicity issues.
• Coumarins, a class of natural compounds, exhibit diverse pharmacological properties, including anti-cancer effects.
• There is a critical need for novel, effective, and safer therapeutic agents against breast cancer.

Purpose of the Study:

• To review the development of coumarin-inspired anti-breast cancer agents over the past three decades.
• To highlight design strategies, mechanistic insights, and structure-activity relationships of these agents.
• To provide a guideline for researchers in developing optimized coumarin-based breast cancer therapies.

Main Methods:

• Comprehensive literature review of coumarin derivatives with anti-breast cancer activity.
• Analysis of published studies focusing on design strategies and structure-activity relationships.
• Inclusion of natural coumarins with demonstrated anti-breast cancer efficacy.

Main Results:

• Numerous synthetic coumarin derivatives have shown significant anti-breast cancer efficacy.
• Key design strategies and mechanistic pathways have been identified.
• Structure-activity relationship studies provide insights into optimizing potency and safety.

Conclusions:

• Coumarin-based compounds represent a promising scaffold for developing novel anti-breast cancer drugs.
• Further research into coumarin derivatives can lead to more potent and safer therapeutic options.
• This review serves as a valuable resource for advancing coumarin-based breast cancer drug discovery.