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2‐Styrylchromones have been shown to possess a broad spectrum of biological activities. Replacing the carbon atom in 2‐styrylchromones with a nitrogen atom in the benzene rings forms 2‐(pyridylvinyl)chromen‐4‐ones (aza‐2‐styrylchromones). We have synthesized a series of novel 2‐(pyridylvinyl)chromen‐4‐ones and their pyridine N‐oxides to evaluate them as potential anticancer agents against human non‐small‐cell...