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Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
Published on: August 14, 2019
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Flavones: an important scaffold for medicinal chemistry
Manjinder Singh1, Maninder Kaur1, Om Silakari1
1Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.
European Journal of Medicinal Chemistry
|July 15, 2014
Summary
Flavones exhibit diverse pharmacological activities, including antioxidant and anti-inflammatory effects, making them crucial for developing new therapeutics. Understanding their structure-activity relationships aids in designing effective treatments for complex diseases.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Biochemistry
Background:
- Flavones possess a wide spectrum of biological activities, including antioxidant, anti-proliferative, anti-tumor, anti-microbial, estrogenic, acetylcholinesterase inhibition, and anti-inflammatory properties.
- These compounds influence mammalian enzymes like protein kinases, which regulate critical cell signaling pathways often dysregulated in various diseases.
- Flavones are recognized as vital scaffolds for the development of novel therapeutic agents, particularly for conditions linked to oxidative stress.
Purpose of the Study:
- To review the detailed structural requirements of flavone derivatives for diverse pharmacological activities.
- To highlight the significance of structure-activity relationships in optimizing flavone-based drug design.
- To provide insights for medicinal chemists in developing selective and poly-functional flavone derivatives for multifactorial diseases.
Main Methods:
- Literature review focusing on flavone derivatives and their pharmacological actions.
- Analysis of structure-activity relationships (SAR) for various biological activities.
- Synthesis and evaluation of flavone derivatives reported in scientific literature.
Main Results:
- Flavones demonstrate significant potential in treating cancer, cardiovascular diseases, and neurodegenerative disorders.
- Recent studies confirm the positive impact of flavones on diseases associated with oxidative stress.
- The development of flavone derivatives for diverse diseases has been rapid, underscoring their therapeutic relevance.
Conclusions:
- Flavone derivatives are indispensable in medicinal chemistry for developing new therapeutic agents.
- Understanding the structural basis of flavone activity is key to designing effective drugs for complex, multifactorial diseases.
- This review provides a foundation for designing optimized flavone derivatives with enhanced selectivity and poly-functionality.
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