The EtOAc and MeOH extracts of the roots of Toddalia asiatica Lam. were investigated for the roots’ chemical constituents. Two new compounds including 2′R-acetoxytoddanol (1) and 8S-10-O-demethylbocconoline (3) as well as 15 known compounds were isolated. Compound 10 showed strong cytotoxicity against KB cells with an IC50 value of 2.60 μg/mL, which is nearly equal to the ellipticine standard, but showed no activity against Vero cells. Alkaloid 3 displayed weak cytotoxicity against the KB cell line with an IC50 value of 21.69 μg/mL. © 2017 Informa UK Limited, trading as Taylor & Francis Group.