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腺嘌呤核苷3’,5’-环磷酸(c-AMP)的磷酸衍生物可能作为c-AMP在体内的模拟物或贮存形式,因此研究c-AMP磷酸衍生物的合成及其生物活性,有可能为发现新药开辟途径.作者曾报道c-AMP的磷酯和磷酰胺的合成,并发现这类衍生物对肿瘤细胞的DNA和RNA的合成有较强抑制作用.本文讨论了含有不同离去基团的三价磷试剂与2’-保护的核苷反应,可以直接环合生成各种核苷3’,5’-环亚磷酸衍生物,后者进一步与碘或硫反应可
Phosphoric acid derivatives of adenosine 3 ’, 5’-cyclophosphate (c-AMP) may serve as in vivo mimic or storage forms of c-AMP. Therefore, the synthesis of c-AMP phosphate derivatives and their biological activity were investigated. It is possible for the discovery of new drugs to open up the way.The authors have reported c-AMP phospholipid and phosphoramidite synthesis and found that such derivatives on tumor cells DNA and RNA synthesis has a strong inhibitory effect.In this paper, The dephosphorylated reagent of the deprotection group reacts with the 2’-protected nucleoside and can be directly cyclized to generate various nucleoside 3 ’, 5’-cyclic phosphorous acid derivatives which react further with iodine or sulfur