ZnCl₂ catalyzed new coumarinyl-chalcones as cytotoxic agents

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Pharmacology

Background:

• Dihydropyrimidinone and coumarin scaffolds are known for diverse biological activities.
• Chalcones are versatile intermediates in organic synthesis with potential therapeutic applications.

Purpose of the Study:

• To design and synthesize novel coumarin-yl-chalcone derivatives.
• To evaluate the in silico and in vitro anti-cancer potential of the synthesized compounds.

Main Methods:

• Multi-component reactions and Claisen-Schmidt condensation were employed for synthesis.
• In silico screening against tyrosine kinases (Src, Alb) and homology model protein.
• In vitro cytotoxic evaluation using MTT assay on A549, Jurkat, and MCF-7 cell lines.

Main Results:

• A series of coumarin-yl-chalcone derivatives (3a-m) were synthesized in good yields.
• Compounds 3h and 3m exhibited moderate binding energies in silico.
• Derivatives 3h and 3m demonstrated significant in vitro anti-cancer activity against tested cell lines, though less potent than Imatinib.

Conclusions:

• The synthesized coumarin-yl-chalcone derivatives hold promise as anti-cancer agents.
• Further optimization may lead to more potent anti-cancer drug candidates.