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Phosphorothioate oligonucleotides containing modified nucleotides with six-membered azasugars and use for AIDS therapy thereof
Phosphorothioate oligonucleotides containing modified nucleotides with six-membered azasugars and use for AIDS therapy thereof
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机译:含有带有六元氮杂糖的修饰核苷酸的硫代磷酸酯寡核苷酸及其在艾滋病治疗中的用途
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摘要
PURPOSE: Provided are phosphorothioate oligonucleotides containing modified nucleotides with six-membered azasugars and their use for AIDS therapy. The phosphorothioate oligonucleotides block HIV attachment, show broad spectrum of anti HIV activity to various HIV mutants and have low toxicity. CONSTITUTION: The phosphorothioate oligonucleotide is represented by the formula(1) in which five-membered ribose is substituted with six-membered azasugar. In the formula, n is an integer of 0-30; B is a natural nucleotide base or a modified nucleotide base with or without a protection group; X is hydrogen, a hydroxyl protection group, a conjugate group or an oligonucleotide; and Y is hydrogen, phosphate, activated phosphate, activated phosphite or a solid support, a conjugate group, an oligonucleotide. The pharmaceutical composition for the AIDS therapy contains the above phosphorothioate oligonucleotide as an active ingredient.
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