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Synthesis and anti-proliferative activity of N,N’-bis-substituted-2,4-triazolium salts with lipophilic and hydrophilic substituents

Abstract

The prevalence of fatalities among cancer patients has stimulated an increased effort to produce more viable anti-cancer therapeutics with fewer side effects. Imidazolium and benzimidazolium salt compounds have been extensively researched due to their promising anti-tumor activities. However, the non-water soluble nature of these two classes of compounds has substantially decreased their viability in the clinical atmosphere. Previously, we reported the anti-proliferative activities of N,N’-bis-substituted 1,2,4-triazolium salts with substituents placed on the N1 and N4 positions, which showed an improvement in anti-proliferative activity while maintaining viable aqueous solubility. To further the understanding of triazolium salts as anti-tumor agents, we present a structure activity relationship (SAR) of N,N’-bis-substituted triazolium salts synthesized from 1,2,3- and 1,2,4-triazole rings with substituents on the C3, N1, and N4 positions. These novel N,N’-bis-substituted triazolium salts will be synthesized, characterized, and tested for their aqueous solubilities and anti-proliferative activities.

Acknowledgements

Columbus State University (CSU) Departments of Chemistry and Biology ; (CSU) Student Resreach and Creative Endevors (SRACE)

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