【摘 要】
：
Pronucleotides are consider as a new generation of anti-HIV pro-drugs.Their main advantage over recently used nucleoside analogues is that they by-pass one of the crucial bioactivation step, namely ph
【机 构】
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Institute of Bioorganic Chemistry,Polish Academy of Sciences Poland
【出 处】
：
2013百奥泰波兰重大疾病临床峰会
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Pronucleotides are consider as a new generation of anti-HIV pro-drugs.Their main advantage over recently used nucleoside analogues is that they by-pass one of the crucial bioactivation step, namely phosphorylation by nucleotide kinase (.e.g.thymidine kinase).All of pronucleotides are properly masked nucleotides what enable them to penetrate and cross cell membrane and in the cell upon chemical or enzymatic hydrolysis are converted into respective nucleoside phosphates and then into di-and finally triphosphates.H-Phosphonates due to exceptional synthetic "flexibility" are very good substrates for synthesis of variety of nucleotide derivatives and/or analogues that bears modification(s) what encourage to consider them as pro-nucleotides.In this presentation, we attempt to summarize our contribution in conceptual and synthetic development of anti-HIV pronucleotides which derived from our studies of H-phosphonates chemistry.Although several type (e.g.nucleoside phosphonate-phosphates or nucleoside α-hydroxyphosphonates) of investigated compounds were found as an exclusive nucleoside vehicles the others (e.g.di-aryl nucleoside phosphotriesters or (N-aryl)phosphoramidates) were proved to act as an efficient anti-HIV pronucleotides.Some aspects of t t-phosphonates chemistry useful in preparation of variety of potential anti-H IV pro-nucleotides will be presented and discussed.
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