Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.

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Chalcone: A Privileged Structure in Medicinal Chemistry.

Coumarins as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies

Current developments of coumarin-based anti-cancer agents in medicinal chemistry

Flavones: An important scaffold for medicinal chemistry

Coumarin heterocyclic derivatives: chemical synthesis and biological activity

Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.

Molecular iodine catalysed one-pot synthesis of chromeno[4,3-b]quinolin-6-ones under microwave irradiation

Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris. In addition, it has showed no cytotoxicity and hemolysis at 10 times the MIC concentration. SAR studies indicate that position of the chlorine atom in the hybrid critically determines the antibacterial activity.

Gopala Reddy Palnati

Papers

Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.

Molecular iodine catalysed one-pot synthesis of chromeno[4,3-b]quinolin-6-ones under microwave irradiation

Coumarin–benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation

Coumarin chalcone fibrates: a new structural class of lipid lowering agents.

Efficient and General Synthesisof 3-Aryl Coumarins Using Cyanuric Chloride