ArticleCurrent pharmaceutical design2025
Synthesis and Structural Characterization of Ferrocenyl Carboxylate Containing Benzaldoxime Moieties and Preliminary Cytotoxicity against Cancer Cell Lines.
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Abstract
aimThis study aimed to design and synthesize new ferrocene derivatives for the development of potent anticancer drugs.
backgroundCancer 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.
methodsFirstly, we synthesized the R-substituted benzaldoxime intermediates (2a-2s) using R-substituted benzaldehyde (1a-1s) and hydroxylamine hydrochloride. Then, the target compounds (3a-3s) were synthesized using ferrocene carboxylic acid and R-substituted benzaldoxime intermediates (2a-2s) 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 in vitro cytotoxicity against HeLa, A549, and A2780 cell lines was evaluated using MTT assay.
resultsThe results showed that compound 3a exhibited cytotoxicity against both HeLa and A549 cancer cell lines with IC
conclusionIn this work, 19 new ferrocene derivatives containing R-substituted benzaldoxime moieties (3a-3s) 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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