Abstract: A new series of camptothecin-inspired heterocycle scaffolds were prepared utilizing a three component one-pot synthetic protocol. Their structures were characterized by ¹H NMR and LC-MS. The acaricidal activities against Tetranychus cinnabarinus were further tested. All the synthesized compounds exhibited different degree of acaricidal activities. Especially, the LC₅₀ values of compounds 4l and 7d against T. cinnabarinus were 25.93 mg/L and 28.16 mg/L, respectively, which were very similar to that of camptothecin (24.55 mg/L). Our study provides a basis for the further development of novel insecticide with camptothecin as the lead compound.