Synthesis of 4'-ethynyl-purine nucleosides possessing anti-HIV activity

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-...

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Bibliographic Details
Published in:Nucleic acids symposium series (1979) 2000 (44), p.105
Main Authors: Kitano, K, Sakata, S, Kohgo, S, Matsuoka, M, Kodama, E, Mitsuya, H, Ohrui, H
Format: Article
Language:English
Subjects:
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
Anti-HIV Agents - toxicity
Cell Death - drug effects
Cell Line
Drug Design
HIV - drug effects
Humans
In Vitro Techniques
Methods
Purine Nucleosides - chemical synthesis
Purine Nucleosides - chemistry
Purine Nucleosides - pharmacology
Purine Nucleosides - toxicity
Structure-Activity Relationship
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Summary: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.
ISSN:0261-3166