Development of Trioxane-Glycolipid Hybrids as Anti-oral Cancer Agents.

D Min, J Ricci, M Kim, WY Chung, KK Park, M Jung. Yonsei University, Chemistry, Republic of Korea

In order to improve anticancer activity, treatment using hybrids drugs, an approach that incorporates two drugs into a single molecule, has been developed. The use of hybrid drugs can impact multiple targets simultaneously. Furthermore, no anti-oral cancer agent has been reported in the literature to date. In this study we report on the practical synthesis and the first potent in vitro anti-oral cancer activity of derivatives of artemisinins, glycolipids, and trioxane-glycolipid hybrids. Novel trioxane-glycolipid hybrids were directly synthesized from 12β(C-C)-type deoxoartemisinin and glycolipid by coupling reaction and exhibited exceptional in vitro anticancer activity, particularly against the oral carcinoma cancer cell lines, HSC-2 and Ca.9-22, respectively. The trioxane-glycolipid hybrids, with effective concentrations under 20 µM, demonstrated better anticancer activity than either artemisinin or glycolipid alone and showed five times more anti-oral cancer activity than either cisplatin or paclitaxel.