Abstract Syringaldehyde was utilized in synthesis of different heterocyclic systems. Some of the synthesized compounds 2 , 7 , 8 , 10 , 11 , and 13 were tested for antioxidant activity where they showed ability to inhibit oxidation in kidney and rat brain homogenates using 2, 2′‐azinobis (3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS). Also, the activity against cancer was examined using the standard MTT method for two human tumor cell lines namely; mammary gland breast cancer MCF‐7 and hepatocellular carcinoma HepG2. The highest activity as antioxidant and antitumor agents was exhibited by compounds 8 and 11 . However, moderate activities were shown by compounds 10 and 13 . While, compounds 2 , 7 showed weak activities.