Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis
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 a...
Saved in:
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Frontiers Media S.A.
2025-01-01
|
| Series: | Frontiers in Chemistry |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fchem.2025.1456743/full |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832589842499764224 |
|---|---|
| author | Zhihong Hu Xixi Hou Yongjing Ren Ziyuan Wu Dong Yan Hong Chen Lan Wang |
| author_facet | Zhihong Hu Xixi Hou Yongjing Ren Ziyuan Wu Dong Yan Hong Chen Lan Wang |
| author_sort | Zhihong Hu |
| collection | DOAJ |
| description | 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 c13-induced apoptosis. In brief, these results indicated that compound c13 is a promising compound for the treatment of cervical cancer. |
| format | Article |
| id | doaj-art-60aced673914460a80576ea5a028020e |
| institution | Kabale University |
| issn | 2296-2646 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Chemistry |
| spelling | doaj-art-60aced673914460a80576ea5a028020e2025-01-24T07:13:49ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462025-01-011310.3389/fchem.2025.14567431456743Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosisZhihong Hu0Xixi Hou1Yongjing Ren2Ziyuan Wu3Dong Yan4Hong Chen5Lan Wang6College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, ChinaThe First Affiliated Hospital, College of Clinical Medicine of Henan University of Science and Technology, Luoyang, ChinaCollege of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, ChinaCollege of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, ChinaCollege of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, ChinaLuoyang Key Laboratory of Organic Functional Molecules, College of Food and Drug, Luoyang Normal University, Luoyang, ChinaCollege of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, ChinaCervical 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 c13-induced apoptosis. In brief, these results indicated that compound c13 is a promising compound for the treatment of cervical cancer.https://www.frontiersin.org/articles/10.3389/fchem.2025.1456743/fullcervical cancergefitinib1,2,3-triazolecell cycleapoptosis |
| spellingShingle | Zhihong Hu Xixi Hou Yongjing Ren Ziyuan Wu Dong Yan Hong Chen Lan Wang Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis Frontiers in Chemistry cervical cancer gefitinib 1,2,3-triazole cell cycle apoptosis |
| title | Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis |
| title_full | Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis |
| title_fullStr | Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis |
| title_full_unstemmed | Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis |
| title_short | Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis |
| title_sort | anti cancer activity of synthetic gefitinib 1 2 3 triazole derivatives against hela cells via induction of apoptosis |
| topic | cervical cancer gefitinib 1,2,3-triazole cell cycle apoptosis |
| url | https://www.frontiersin.org/articles/10.3389/fchem.2025.1456743/full |
| work_keys_str_mv | AT zhihonghu anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT xixihou anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT yongjingren anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT ziyuanwu anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT dongyan anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT hongchen anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis AT lanwang anticanceractivityofsyntheticgefitinib123triazolederivativesagainsthelacellsviainductionofapoptosis |