1. 2′,3′-Dideoxyuridine triphosphate conjugated to SiO 2 nanoparticles: Synthesis and evaluation of antiproliferative activity
- Author
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Svetlana V. Vasilyeva, Inga R. Grin, Dmitry A. Stetsenko, and Boris P. Chelobanov
- Subjects
0301 basic medicine ,chemistry.chemical_classification ,010405 organic chemistry ,Organic Chemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Conjugated system ,01 natural sciences ,Biochemistry ,0104 chemical sciences ,03 medical and health sciences ,030104 developmental biology ,chemistry ,Drug Discovery ,Cancer cell ,Click chemistry ,Molecular Medicine ,Phosphorylation ,Nucleotide ,Cytotoxicity ,Molecular Biology ,Nucleoside ,Conjugate - Abstract
A conjugate of triphosphorylated 2′,3′-dideoxyuridine (ddU) with SiO2 nanoparticles was obtained via the CuAAC click chemistry between a γ-alkynyl ddU triphosphate and azido-modified SiO2 nanoparticles. Assessment of cytotoxicity in human breast adenocarcinoma MCF7 cells demonstrated that ddU triphosphate conjugated to SiO2 nanoparticles exhibited a 50% decrease in cancer cell growth at a concentration of 183 ± 57 µg/mL, which corresponds to 22 ± 7 µM of the parent nucleotide, whereas the parent nucleoside, nucleotide and alkynyl triphosphate precursor do not show any cytotoxicity. The data provide an example of remarkable potential of novel conjugates of SiO2 nanoparticles with phosphorylated nucleoside analogues, even those, which have not been used previously as therapeutics, for application as new anticancer agents.
- Published
- 2018
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