Chemotherapy is recognized as one of the indispensable treatment for solid tumors. However, the emergent drug resistance and undesirable side effects have become a substantial challenge and the bottleneck of cancer chemotherapy. Magnolol (MAG) is a natural polyphenol with various bioactivities. Sulforaphane (SFN) is identified as one of the most effective naturally occurring anticancer agents. In this study, we successfully synthesized the magnolol-sulforaphane (MAG-SFN) hybrid CT1-3, showcasing more efficient anticancer activity than its lead compounds MAG and SFN with IC<sub>50</sub> values ranging from 5.10 to 14.06 μM in multiple cancer cells. We also demonstrated that CT1-3 elicited a strong antitumor effect in vivo but has no hepatic and renal toxicity. Furthermore, we found out CT1-3 treatment resulted in reduction of Bcl-2 and XIAP levels, in addition to increase of phospho-JNK and Bax levels, leading to mitochondria-mediated apoptosis in human cancer cells. Moreover, we revealed that CT1-3 could reduce the capacity of migration and invasion of human cancer cells via regulating the E-cadherin/Snail axis. Taken together, we provided strong evidences that the first example of MAG-SFN hybrid CT1-3 is a promising anticancer drug candidate without apparent adverse effects, which suppresses tumorigenesis partly through inducing mitochondria-mediated apoptosis and inhibiting epithelial mesenchymal transition (EMT).