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

Abstract

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.

Keywords: Anti-cancer activity; Click chemistry; Copper(I) oxide nanoparticles; Melampomagnolide B; Parthenolide.