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ORIGINAL RESEARCH article
Front. Pharmacol.
Sec. Pharmacology of Anti-Cancer Drugs
Volume 16 - 2025 | doi: 10.3389/fphar.2025.1565657
Synthesis, Anti-cancer Activity, and Mechanistic Insights of 2H-benzo[b][1,4]oxazin-3(4H)-one Linked 1,2,3-Triazoles in Human Cancer Cell Lines
Provisionally accepted- 1Department of Pain Management, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, China
- 2The First Affiliated Hospital of Henan University of Science and Technology, Luoyang, China
- 3Macao Polytechnic University, Macau, Macao, SAR China
- 4The Eighth Affiliated Hospital, Sun Yat-sen University, Shenzhen, China
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A series of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives linked to 1,2,3-triazoles were designed, synthesized, and evaluated for their anticancer activity in several human cancer cell lines, including A549 (lung), Huh7 (liver), MCF-7 (breast), , and SKOV3 (ovary). Cell viability assays revealed that these compounds exhibited the most potent activity against A549 cells. Among them, compounds 14b and 14c demonstrated the strongest inhibitory effects, with IC50 values of 7.59±0.31 μM and 18.52±0.59 μM, respectively. Flow cytometry analysis further confirmed that compounds 14b and 14c induced significant apoptosis.Additional studies showed that these compounds elevated reactive oxygen species (ROS) levels, which may contribute to apoptosis. Moreover, compounds 14b and 14c notably increased the number of dead cells while reducing viable cell counts. Western blot analysis indicated that these compounds could induce DNA damage and autophagy, which may play a key role in their anticancer effects.
Keywords: anticancer, Apoptosis, 2H-benzo[b][1,4]oxazin-3(4H)-one, 1,2,3-triazole, ROS, DNA Damage
Received: 23 Jan 2025; Accepted: 09 Apr 2025.
Copyright: © 2025 Liu, Hou, Tian, He, Guo, Guo and Yang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Xixi Hou, The First Affiliated Hospital of Henan University of Science and Technology, Luoyang, China
Jianxue Yang, The First Affiliated Hospital of Henan University of Science and Technology, Luoyang, China
Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.