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Forty-two 3-substituted 1-(5-formylfurfuryl)indolin-2-ones were synthesized and most of these compounds exhibited potent inhibitory activities against P. oryzae (MIC = 0.78-25 μg/mL) and human intestinal Caco-2 cells (IC50 = 0.19-9.42 μM). Eight compounds selected for further screening also showed inhibitory activities (IC50 = 1.84-10.32 μM) against human lung adenocarcinoma cells (SPC-A1).