Nine new ent-kaurane diterpenoids, isoscoparins D-L (1-9), and an artificial product, the acetonide of rabdoloxin A (10), along with 16 known analogues (11-26), were isolated from the leaves of Isodon scoparius. The new structures were determined by 1D and 2D NMR spectroscopic analysis. Selected compounds were evaluated for their cytotoxicity against NB4, A549, PC-3, MCF-7, and SH-SY5Y cell lines.