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Current Bioactive Compounds

Author(s): Mohamed Abdelkarim*, Khaoula Ben Younes, Ines Limam, Refka Guermazi, Amel Ben Ammaar ElGaaied and Fatma Ben Aissa-Fennira

DOI: 10.2174/1573407215666181224105826

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3,6-dichloro-1,2,4,5-Tetrazine Assayed at High Doses in the Metastatic Breast Cancer Cell Line MDA-MB-231 Reduces Cell Numbers and Induces Apoptosis

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Abstract

Background: The lack of treatment options for patients with chemotherapy-resistant cancers is pushing the field toward the development of new therapies. 1,2,4,5-tetrazine derivatives are a class of heterocyclic compounds that exhibit a broad spectrum of antitumor activities.

Objective: The purpose of this study was to assess the biological activity of four s-tetrazine derivatives by substitution of two chloride atom of 3,6-dichloro-1,2,4,5-tetrazine with long hydrophobic side chains.

Methods: We analyzed the anti-proliferative effects of four s-tetrazine derivatives with MTT assay and their pro-apoptotic effect with AV/ IP flow cytometry analysis and Hoechst 33342 staining.

Results: We demonstrated that 3,6-dichloro-1,2,4,5-tetrazine (compound (1)) has a cytotoxic effect and induces apoptosis.

Conclusion: 3,6-dichloro-1,2,4,5-tetrazine presents a new cytotoxic drug against metastatic breast cancer cell line MDA-MB-231 in vitro.

Keywords: 1, 2, 4, 5-tetrazine derivatives, in vitro experiment, MDA-MB-231 cell line, breast cancer, 3, 6-dichloro-1, 2, 4, 5- tetrazine, apoptosis.

Graphical Abstract

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