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A series of 4 0 -N-substituted (aminomethyl)benzoate derivatives of scutellarein were designed and synthesized. Evaluation of their physiochemical properties showed that the designed target compounds 5a-e exhibit higher chemical stability and aqueous solubility than scutellarin and scutellarein. The permeability (P app AP to BL ) of 5c-e in Caco-2 cells were 2.8, 8.1, and 12.6 times higher than that of scutellarin and 1.3, 4.1, and 6.0 times higher than that of scutellarein; especially, 5e had the highest P app AP to BL value (7.19 ± 0.31 × 10 −6 cm/s) and the lowest ER (P app BL to AP /P app AP to BL ) value of 0.17. In vitro antioxidative evaluation results revealed that 5e could protect against H 2 O 2 -induced PC12 cells' oxidative damage by attenuating mitochondrial membrane potential loss and decreasing H 2 O 2 -induced reactive oxygen species (ROS) production. Result and DiscussionChemistry. The general procedure for the synthesis of 4 0 -Nsubstituted (aminomethyl)benzoate derivatives of scutellarein (5a-e) is outlined in Scheme 1. Scutellarin (1) was treated with 8% dilute aqueous solution of sulfuric acid at 90 C, followed by filtration, drying, and extraction with acetone to give scutellarein 2 in good yield (65%), which was then treated with ¶ These authors have equally contributed to this work.