Synthesis of New Heterocyclic Amino Derivatives of Alantolactone and Their Cytotoxic Activity

In this study, a series of new alantolactone (AL) amino scaffolds (AL1-AL13) had been synthesized and evaluated for in vitro cytotoxicity against three human cancer cell lines: human cervical cancer (SiHa), human epidermoid carcinoma (KB), and human lung cancer (A549). The compounds AL 2, 4, 5, 7, and 13 were found to be nearly as equally active as AL against three tested cell lines, whereas AL 1 and 12 against SiHa cells. This study also provides a correlation on the structure activity relationship of AL and derivatized analogues against tested cells. The retention of cytotoxicity with enhanced water solubility in derivatized amino adducts including AL 1, 2, 4, 5, 7, 12, and 13 indicates that these adducts can further be tested for the detailed in vivo safety and anticancer studies.