改性核苷8-溴腺苷及其磷脂衍生物的合成

SAKHAROV READINGS 2021: ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY Part 2 Pub Date : 2021-05-20 DOI:10.46646/sakh-2021-2-20-23

L. Birichevskaya, M. Vinter, A. A. Doroshevich, M. Khancheuski, E. Kvasyuk, A. Zinchenko

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引用次数: 0

摘要

具有高反应能力的修饰核苷8-溴腺苷可作为合成大量嘌呤抗代谢产物的基础化合物，对多种肿瘤和病毒性疾病具有潜在的治疗活性。在本研究中，8-溴腺苷是在溴水溶液处理核苷前体腺苷后，通过一个简单的生态友好的程序产生的。在酶促转磷脂酰化反应过程中，首次合成了上述核苷-5′-(1,2-二肉豆醇磷脂酰)-8-溴腺苷的磷脂衍生物。新化合物可能作为生物活性抗代谢产物的无毒前体用于药物配方中。

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SYNTHESIS OF THE MODIFIED NUCLEOSIDE 8-BROMADENOSINE AND ITS PHOSPHOLIPID DERIVATIVE

Modified nucleoside 8-bromoadenosine possessing high reactive capacity may serve as a basic compound for the synthesis of a large number of purine antimetabolites showing potentially therapeutic activities toward several tumor and viral diseases. In this study, 8-bromoadenosine was produced by a simple eco-friendly procedure following the treatment of nucleoside precursor adenosine with aqueous bromine solution. In the course of enzymatic transphosphatidylation reaction, the first synthesis of phospholipid derivative of the above-mentioned nucleoside -5‘-(1,2-dimyristoyl phosphatidyl)-8-bromoadenosine was accomplished. Novel compounds may presumably act as non-toxic progenitors of bioactive antimetabolites to be used in drug formulas.

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SAKHAROV READINGS 2021: ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY Part 2

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