1434271-16-5Relevant articles and documents
Synthesis and biological evaluation of novel 1,2,3-triazolonucleotides
Glowacka, Iwona E.,Balzarini, Jan,Wroblewski, Andrzej E.
, p. 278 - 291 (2013/06/04)
A general procedure for the preparation of 1,2,3-triazole analogs of nucleosides from diethyl 2-azidoethoxymethyl- and 2-azidoethoxyethylphosphonates was elaborated. The application of microwave irradiation shortened the reaction time to 10 min in comparison to ca. 48 h when 1,3-dipolar cycloadditions were performed under standard conditions. All compounds were evaluated in vitro for inhibitory activity against a broad variety of DNA and RNA viruses. None of the compounds were antivirally active at subtoxic concentrations. Compound 17k exhibited moderate inhibitory effects on the proliferation of human T-lymphocyte cells (IC50 = 64 μM for CEM). The inhibitory activity of cell proliferation for HEL cells as well as L1210, CEM, and HeLa cells of several 1,2,3-triazole analogs of nucleotides was evaluated. The 1,2,3-triazole derivatives appeared to be cytostatic (with IC50 values reaching the middle to higher micromolar range: 60-250 μM). Copyright
