Nucleoside dimers analogues with a 1,2,3-triazole linkage: conjugation of floxuridine and thymidine provides novel tools for cancer treatment. Part II

Abstract

The fluorinated nucleoside dimers with a 1,2,3-triazole linkage are novel compounds within the field of bioorganic chemistry. We report on the synthesis and properties of two groups of nucleoside dimers analogs possessing a different arrangement of the 1,4-disubstituted 1,2,3-triazole linkage. Based on analysis of the ³J_HH, ³J_H1′C2, and ³J_H1′C6 we estimated conformational preferences of sugar part and orientation around glycosidic bond. These compounds show moderate anticancer activity, with cytostatic studies in three different cancer cell lines.

Keywords:

• Floxuridine
• nucleoside dimers derivatives
• 1,3-dipolar cycloaddition
• cancer therapy

Acknowledgments

We are grateful to Prof. Maciej Stobiecki for ME ES analysis of novel compounds. Financial support from the Polish Ministry of Science and Higher Education (statutory financing and the KNOW program), is greatfully acknowledged.

Additional information

Funding

Financial support from the Polish Ministry of Science and Higher Education (statutory financing and the KNOW program), is greatfully acknowledged.