To further understand the chemotaxonomy of the genus Cananga and to continue searching for novel bioactive agents from Annonaceous plants,6 C. odorata was chosen for the present phytochemical investigation. In this paper, we report the isolation and characterization of four compounds, including one new guaipyridine sesquiterpene alkaloid, cananodine (1), two new eudesmane sesquiterpenes, cryptomeridiol 11-R-L-rhamnoside (2) and γ-eudesmol 11-R-L-rhamnoside (3), along with one known12 eudesmane sesquiterpene, γ-eudesmol (4), which was isolated for the first time from this plant. The structures of the new compounds 1-3 were established on the basis of NMR and MS data interpretation. Furthermore, compounds 1-4 and four previously reported alkaloids6 from this plant, cleistopholine (5), N-trans-feruloyltyramine (6), (+)-ushinsunineâ-N-oxide (7), and lyscamine (8), were evaluated for their cytotoxicity against two human hepatocarcinoma cell lines.