Synthesis and biological evaluation of triazole and isoxazole-tagged benzothiazole/benzoxazole derivatives as potent cytotoxic agents

Abstract

Cancer is a major health problem and the most upsetting disease in humans, leading to death in both developed and developing countries. Proper treatment of the disease is still a challenge. Chemotherapy is considered one of the regimens to cure this disease. In this study, a series of 1,2,3-triazole and isoxazole-linked benzothiazole/benzoxazole derivatives were synthesized and evaluated for their anticancer activity against human cancer cell lines, such as HeLa (cervical), and A549 (lung) cell lines, with HEK-293 cell line used as a control. Among them, conjugates 8a, 8f, 13g, 13h and 13j displayed significant cytotoxic activity against human cancer cell lines. Furthermore, these active conjugates induced an increase in the expression of key apoptotic genes that are involved in the intrinsic pathway of apoptosis such as caspase-9, caspase-3, BAX and cytochrome-c. This study may provide possible anti-cancer therapeutics against HeLa and lung cancer cells.