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2000
Volume 31, Issue 31
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

Aim

This study aimed to design and synthesize new ferrocene derivatives for the development of potent anticancer drugs.

Background

Cancer is a major cause of death globally. Some small-molecule anticancer drugs have been used in clinics for the treatment of cancer, and several candidates are in different phases of clinical trials. However, cancer chemotherapy is still highly inadequate due to the side effects of the clinical drugs. Thus, developing novel anticancer drugs is essential.

Methods

Firstly, we synthesized the R-substituted benzaldoxime intermediates () using R-substituted benzaldehyde () and hydroxylamine hydrochloride. Then, the target compounds () were synthesized using ferrocene carboxylic acid and R-substituted benzaldoxime intermediates () as starting materials, and using DCC and DMAP as catalysts. The purity of the target compounds was determined by HPLC, and their structures were characterized using NMR, SC-XRD, and HR-ESIMS. Subsequently, the preliminary cytotoxicity against HeLa, A549, and A2780 cell lines was evaluated using MTT assay.

Results

The results showed that compound exhibited cytotoxicity against both HeLa and A549 cancer cell lines with IC values of 0.691 and 0.876 mM, respectively. Compound showed potent cytotoxicity against HeLa cell lines with an IC value of 0.097 mM, compounds and exhibited potent cytotoxicity against three cancer cell lines, compound showed potent cytotoxicity against HeLa cell lines with an IC value of 0.175 mM, while compound exhibited potent cytotoxicity against HeLa and A549 cell lines with IC values of 0.470 and 0.298 mM, respectively.

Conclusion

In this work, 19 new ferrocene derivatives containing R-substituted benzaldoxime moieties (-) were synthesized and their structures were confirmed. Their cytotoxicity against HeLa, A549, and A2780 cell lines was tested, and the results showed that several compounds exhibited potent cytotoxicity against the tested cancer cell lines. This work developed a variety of ferrocene compounds, providing lead compounds based on ferrocene pharmacophore for the development of anticancer drugs.

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2025-05-08
2025-08-18

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Synthesis and Structural Characterization of Ferrocenyl Carboxylate Containing Benzaldoxime Moieties and Preliminary Cytotoxicity against Cancer Cell Lines
Curr. Pharm. Des. 31, 2537 (2025); https://doi.org/10.2174/0113816128391868250430081054
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  • Article Type:     Research Article
Keyword(s): benzaldoxime moieties; cancer cell lines; crystal structure; cytotoxicity; Ferrocenyl carboxylates; synthesis

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