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

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

  • Eur J Med Chem. 2018 Aug 5:156:216-229. doi: 10.1016/j.ejmech.2018.06.058.
Yahui Ding 1,  Hongyu Guo 1,  Weizhi Ge 1,  Xinyi Chen 1,  Shengzu Li 1,  Mengmeng Wang 2,  Yue Chen 1,  Quan Zhang 3
Affiliations

Affiliations

  • 1 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.
  • 2 Accendatech Company, Ltd., Tianjin, 300384, People's Republic of China.
  • 3 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: zhangquan@nankai.edu.cn.
PMID: 30006167 DOI: 10.1016/j.ejmech.2018.06.058
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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z