Ongoing search for promising antitumor components from plant resources, we found that the methanol extract from the heartwood of Dalbergia odorifera (Leguminosae) demonstrated a significant inhibition on the proliferation of human tumor cell lines including multidrug resistant cells in vitro. Intensive bioassay-guided purification of the extract finally led to the isolation of seven flavonoids and two phenolic components as active constituents for antitumor property, in vitro, i.e., medicarpin (1), 2-hydroxy-3,4-dimethoxybenzaldehyde (2), formononetin (3), tectorigenin (4), mucronulatol (5), (3R)-5′-methoxyvestitol (6), hydroxyobtustyrene (7), liquiritigenin (8), and (3R)-calussequinone (9), respectively.