# Mechanistic Insights and Anti-cancer Activity of 2H-benzo[b][1,4]oxazin-3(4H)-one Linked 1,2,3-Triazoles in Human Cancer Cells

**Authors:** Qingying Liu, Xixi Hou, Mingyue Tian, Baoyu He, Jingjing Guo, Yajie Guo, Jianxue Yang

PMC · DOI: 10.3389/fphar.2025.1565657 · Frontiers in Pharmacology · 2025-06-13

## TL;DR

This study designed and tested new compounds that show strong anti-cancer effects, especially in lung cancer cells, by inducing cell death and DNA damage.

## Contribution

The paper introduces novel 2H-benzo[b][1,4]oxazin-3(4H)-one linked 1,2,3-triazoles with potent anti-cancer activity and provides mechanistic insights into their action.

## Key findings

- Compounds 14b and 14c showed the strongest anti-cancer activity against A549 lung cancer cells with IC50 values of 7.59 μM and 18.52 μM.
- These compounds induced apoptosis and increased reactive oxygen species (ROS) levels in cancer cells.
- Western blot analysis revealed that the compounds caused DNA damage and autophagy, contributing to their anti-cancer effects.

## Abstract

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), HCT-116 (colon), 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.

## Linked entities

- **Chemicals:** 2H-benzo[b][1,4]oxazin-3(4H)-one (PubChem CID 72757)
- **Diseases:** lung cancer (MONDO:0005138), liver cancer (MONDO:0002691), breast cancer (MONDO:0004989), colon cancer (MONDO:0002032), ovary cancer (MONDO:0008170)
- **Species:** Homo sapiens (taxon 9606)

## Full-text entities

- **Diseases:** Cancer (MESH:D009369)
- **Chemicals:** ROS (MESH:D017382), 2H-benzo[b][1,4] oxazin-3(4H)-one (MESH:C000724153), 1,2,3-Triazoles (-)
- **Species:** Homo sapiens (human, species) [taxon 9606]
- **Cell lines:** SKOV3 — Homo sapiens (Human), Ovarian serous cystadenocarcinoma, Cancer cell line (CVCL_0532), A549 — Homo sapiens (Human), Lung adenocarcinoma, Cancer cell line (CVCL_0023), HCT-116 — Homo sapiens (Human), Colon carcinoma, Cancer cell line (CVCL_0291), MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031), Huh7 — Homo sapiens (Human), Adult hepatocellular carcinoma, Cancer cell line (CVCL_0336)

## Full text

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## Figures

12 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12202533/full.md

## References

26 references — full list in the complete paper: https://tomesphere.com/paper/PMC12202533/full.md

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Source: https://tomesphere.com/paper/PMC12202533