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.
Accendatech Company, Ltd., Tianjin, 300384, People's Republic of China.
Eur J Med Chem. 2018 Aug 5;156:216-229. doi: 10.1016/j.ejmech.2018.06.058. Epub 2018 Jun 25.
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.
通过氧化铜纳米粒子催化的点击化学，合成了一系列三十一烯丙醇 B-三唑缀合物。评估了这些缀合物对五种人癌细胞系的抗癌活性。最活性化合物 6e 对 HCT116 细胞系表现出高活性，IC 值为 0.43 μM，与母体化合物 melampomagnolide B（IC = 4.93 μM）相比提高了 11.5 倍。化合物 6e 显示出诱导细胞凋亡、抑制 HCT116 细胞增殖和迁移的显著功效。还研究了 6e 的初步分子机制。基于这些结果，化合物 6e 可能被认为是进一步作为潜在抗癌药物进行评估的有前途的候选物。
