Homoisoflavonoids: Synthesis and Biological Activities
Summary
Homoisoflavonoids represent a distinctive subclass of naturally occurring flavonoid derivatives characterised by a 16-carbon skeleton featuring a 3-benzylidene-4-chromanone core. Their unique structure imparts a range of biological activities including antiangiogenic, anti-inflammatory, antioxidant and antimicrobial effects. Synthetic approaches to these compounds have evolved to encompass both linear and convergent strategies, often beginning from readily available chromenone precursors. Modern methods employ chemoselective reductions, regioselective functional-group interconversions and strategic deprotection steps to access substituted 3-benzyl-4-chromanones and related analogues. Advances in chemical proteomics have further facilitated the elucidation of molecular targets through biotin tagging and affinity-based pull-down assays, revealing interactions with key enzymes involved in inflammation, angiogenesis and metabolic regulation. Collectively, synthetic innovations coupled with sophisticated target-identification techniques have bolstered the development of homoisoflavonoid scaffolds as promising leads for therapeutic intervention in oncology, ocular diseases and chronic inflammatory conditions.
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Homoisoflavonoids: Synthesis and Biological Activities publication trend
The graph below shows the total number of articles in homoisoflavonoids: synthesis and biological activities across all publications each year (not limited to Nature Index journals).
Technical terms
Homoisoflavonoid: A flavonoid derivative with a 16-carbon framework, typically featuring a 3-benzylidene-4-chromanone core.
Chemoselective reduction: A chemical transformation that selectively reduces one functional group in the presence of others.
Biotin probe: A biotin-conjugated small molecule used in chemical proteomics to capture and identify protein binding partners.
Chemotaxonomy: The study of chemical variation among plant taxa to understand phylogenetic relationships and guide compound discovery.
References
- Exploring the Antiangiogenic and Anti-Inflammatory Potential of Homoisoflavonoids: Target Identification Using Biotin Probes. Biomolecules (2024).
- A Comprehensive Review on Chemotaxonomic and Phytochemical Aspects of Homoisoflavonoids, as Rare Flavonoid Derivatives. International Journal of Molecular Sciences (2021).
- Synthesis of Natural Homoisoflavonoids Having Either 5,7-Dihydroxy-6-methoxy or 7-Hydroxy-5,6-dimethoxy Groups. Molecules (2016).
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