Synthesis and biological evaluation of novel 1,2,3-triazolonucleotides

G?owackaI.E.; BalzariniJ.; Wr?blewskiA.E.

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Synthesis and biological evaluation of novel 1,2,3-triazolonucleotides

机译：新型1,2,3-三唑并核苷酸的合成与生物学评价

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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).

机译：阐述了由2-叠氮基乙氧基甲基-和2-叠氮基乙氧基乙基膦酸二乙酯制备核苷的1,2,3-三唑类似物的一般程序。相比于大约1℃，微波辐射的应用将反应时间缩短到10分钟。在标准条件下进行1,3-偶极环加成反应后48小时。在体外评估了所有化合物对多种DNA和RNA病毒的抑制活性。在亚毒性浓度下，没有一种化合物具有抗病毒活性。化合物17k对人T淋巴细胞的增殖具有中等抑制作用（对于CEM，IC50 = 64μM）。评估了几种1,2,3-三唑核苷酸类似物对HEL细胞以及L1210，CEM和HeLa细胞的细胞增殖抑制活性。 1,2,3-三唑衍生物似乎具有细胞生长抑制作用（IC50值达到中等至更高的微摩尔范围：60-250μM）。

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《Archiv der Pharmazie》 |2013年第4期|共14页
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G?owackaI.E.; BalzariniJ.; Wr?blewskiA.E.;
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中图分类药学;
关键词
1; 2; 3-Triazoles; Antiviral; Aziodophosphonates; Cycloaddition; Cytostatic;

机译：1;2;3-三唑;抗病毒;偶氮膦酸酯;环加成;细胞抑制剂;

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Synthesis and biological evaluation of novel 1,2,3-triazolonucleotides

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