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A simple, inexpensive, and efficient one-pot synthesis of 1,4-dihydropyridine derivatives was achieved in good yields via the three-component reaction of aromatic aldehydes, ethyl acetoacetate, and ammonium acetate using PhB(OH) 2 as catalyst.

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Aim: There is a continuous and urgent need for new anticancer agents with novel structures and target selectivity. Methods & results: The anticancer activity of the prepared compounds was assessed against human lung (A549) and stomach (AGS) cancer cell lines and evaluated in the noncancer human lung fibroblast (MRC-5) cell line. 2-Pyrazolines were devoid of toxicity in all cell lines used, chalcones bearing a β-(benz)imidazole moiety being toxic toward AGS cell line. Mechanistic studies showed that these compounds trigger loss of cell viability and mitochondrial membrane potential, while eliciting morphological traits compatible with regulated cell death, which was ultimately shown to derive from caspase activation, specifically caspase-3. Conclusion: Chalcones 1–3 have been identified as new and promising anticancer agents toward the AGS cell line.