Copper(I) oxide nanoparticles catalyzed click chemistry based synthesis of melampomagnolide B-triazole conjugates and their anti-cancer activities

• DOI: 10.1016/j.ejmech.2018.06.058
• Publication Date: 2018-06-25T12:39:02Z
• Authors: Yahui Ding; Hongyu Guo; Weizhi Ge; Xinyi Chen; Shengzu Li; Mengmeng Wang; Yue Chen; Quan Zhang
• Keywords: 0303 health sciences; Antineoplastic Agents; Apoptosis; Oxides; Triazoles; HCT116 Cells; Catalysis; 3. Good health; 03 medical and health sciences; Colonic Neoplasms; Humans; Nanoparticles; Click Chemistry; Drug Screening Assays, Antitumor; Sesquiterpenes; Copper; Cell Proliferation

A series of thirty one melampomagnolide B-triazole conjugates was synthesized via Copper(I) oxide nanoparticles catalyzed click chemistry. These conjugates were evaluated for their anti-cancer activities against a panel of five human cancer cell lines. The most active compound 6e showed high activity against HCT116 cell line with IC50 value of 0.43 μM, which demonstrated 11.5-fold improvement compared to that of the parent compound melampomagnolide B (IC50 = 4.93 μM). Compound 6e showed significant efficacy of inducing apoptosis, inhibiting proliferation and migration of HCT116 cells. The preliminary molecular mechanism of 6e was also investigated. On the base of these results, compound 6e might be considered as a promising candidate for further evaluation as a potential anti-cancer drug.