Abstract
A series of novel 1,3,4-oxadiazole-artemisinin hybrids have been designed and synthesized. An MTT assay revealed that most of tested hybrids showed more enhanced anti-proliferative activities than artemisinin, among which A8 had the superior potency with IC50 values ranging from 4.07 μM to 9.71 μM against five tested cancer cell lines. Cell colony formation assays showed that A8 could inhibit significantly more cell proliferation than artemisinin and 5-fluorouracil. Further mechanism studies reveal that A8 induces apoptosis and ferroptosis in MCF-7 cells in a dose-dependent manner, and CYPs inhibition assays reveal that A8 has a moderate inhibitory effect on CYP1A2 and CYP3A4 in the human body at 10 μM. The present work indicates that hybrid A8 may merit further investigation as a potential therapeutic agent.
Funder
National Natural Science Foundation of China
Subject
Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Computer Science Applications,Spectroscopy,Molecular Biology,General Medicine,Catalysis
Reference29 articles.
1. Cancer genes and the pathways they control;Vogelstein;Nat. Med.,2004
2. HPV-associated oropharyngeal cancer: Epidemiology, molecular biology and clinical management;Lechner;Nat. Rev. Clin. Oncol.,2022
3. Cancer statistics, 2021;Siegel;CA Cancer J. Clin.,2021
4. Najmi, A., Javed, S.A., Al Bratty, M., and Alhazmi, H.A. (2022). Modern approaches in the discovery and development of plant-based natural products and their analogues as potential therapeutic agents. Molecules, 27.
5. Natural product anticipation through synthesis;Hetzler;Nat. Rev. Chem.,2022
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献