具有抗HIV活性的4'-乙炔基嘌呤核苷的合成。
Synthesis of 4'-ethynyl-purine nucleosides possessing anti-HIV activity.
作者信息
Kitano K, Sakata S, Kohgo S, Matsuoka M, Kodama E, Mitsuya H, Ohrui H
机构信息
Biochemicals Division, Yamasa Corporation, 2-10-1 Araoicho, Choshi, Chiba 288-0056, Japan.
出版信息
Nucleic Acids Symp Ser. 2000(44):105-6. doi: 10.1093/nass/44.1.105.
PMID:12903290
Abstract
Searching for more effective anti-HIV agents, we have prepared 4'-ethynyl-purine nucleosides. They were derived in several steps from 4-C-triethylsilylethynyl ribose, which was used as an intermediate in the synthesis of pyrimidine nucleosides. The adenine derivative exhibited significant anti-HIV activity and favorable cytotoxicity profile in vitro.
摘要
为了寻找更有效的抗HIV药物，我们制备了4'-乙炔基嘌呤核苷。它们是由4-C-三乙基硅乙炔基核糖经几步反应衍生而来的，4-C-三乙基硅乙炔基核糖在嘧啶核苷的合成中用作中间体。腺嘌呤衍生物在体外表现出显著的抗HIV活性和良好的细胞毒性特征。
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