Discovery of artemisinin-glycolipid hybrids as anti-oral cancer agents

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Authors: Jérémy RICCI ; Minkyu KIM ; Won-Yoon CHUNG ; Kwang-Kyun PARK ; Mankil JUNG

MeSH: Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry* ; Antineoplastic Agents/pharmacology* ; Artemisia/chemistry ; Artemisinins/chemical synthesis ; Artemisinins/chemistry* ; Artemisinins/pharmacology* ; Carcinoma/drug therapy ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Glycolipids/chemical synthesis ; Glycolipids/chemistry* ; Glycolipids/pharmacology* ; Humans ; Mouth Neoplasms/drug therapy ; Neoplasms/drug therapy

Abstract: Novel artemisinin-glycolipid hybrids were directly synthesized from 12β (C-C)-type deoxoartemisinin and glycolipid and exhibited exceptional in vitro anticancer activity, particularly against the oral carcinoma cancer cell lines, respectively. The artemisinin-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