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ORIGINAL RESEARCH article

Front. Chem.
Sec. Medicinal and Pharmaceutical Chemistry
Volume 13 - 2025 | doi: 10.3389/fchem.2025.1456743
This article is part of the Research Topic Five-membered Ring Heterocyclic Compounds as Anticancer Drug Candidates View all 6 articles

Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivative against Hela cells via induction of apoptosis

Provisionally accepted
Zhihong Hu Zhihong Hu 1Xixi Hou Xixi Hou 2*Yongjing Ren Yongjing Ren 1Ziyuan Wu Ziyuan Wu 1Dong Yan Dong Yan 1Hong Chen Hong Chen 3Lan Wang Lan Wang 1*Longfei Mao Longfei Mao 1*
  • 1 Henan University of Science and Technology, Luoyang, China
  • 2 The First Affiliated Hospital of Henan University of Science and Technology, Luoyang, Henan Province, China
  • 3 School of Food and Pharmaceutical Sciences, Luoyang Normal University, Luoyang, Henan Province, China

The final, formatted version of the article will be published soon.

    Cervical cancer ranks as the fourth most common cancer among women. However, the current treatments have significant side effects and limited therapeutic effects on advanced diseases, so it is necessary to discover better treatments for cervical cancer. The current study investigated the potential anticancer effects of a series of gefitinib-1,2,3-triazole derivative on Hela cells. Among the investigated, the target compound c13 showed good anticancer activity against Hela cells (IC50= 5.66 ± 0.35 μM) compared with gefitinib (IC50= 14.18±3.19 μM).Moreover, compound c13 significantly inhibited the colony formation ability of Hela cells in a dose-dependent manner, accompanied by morphological changes in HeLa cells. Further investigations demonstrated that compound c13 triggered cell apoptosis and arrested the cell cycle at the G2/M phase in Hela cells. In addition, western blot analysis revealed that compound c13 upregulated the Bax/Bcl-2 ratio, and increased the levels of active caspase 3 and PARP1 cleavage, which suggested the involvement of the mitochondrial pathway in compound c13induced apoptosis. In brief, these results indicated that compound c13 is a promising compound for the treatment of cervical cancer.

    Keywords: cervical cancer, gefitinib, 1,2,3-triazole, Cell Cycle, Apoptosis

    Received: 29 Jun 2024; Accepted: 06 Jan 2025.

    Copyright: © 2025 Hu, Hou, Ren, Wu, Yan, Chen, Wang and Mao. 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, Henan Province, China
    Lan Wang, Henan University of Science and Technology, Luoyang, China
    Longfei Mao, Henan University of Science and Technology, Luoyang, China

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