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

Eur J Med Chem

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin, 300353, People's Republic of China. Electronic address:

Published: August 2018

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 IC value of 0.43 μM, which demonstrated 11.5-fold improvement compared to that of the parent compound melampomagnolide B (IC = 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.

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Source
http://dx.doi.org/10.1016/j.ejmech.2018.06.058DOI Listing

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