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-HIV activity and favorable cytotoxicity profile in vitro.
Kitano
K
K
Biochemicals Division, Yamasa Corporation, 2-10-1 Araoicho, Choshi, Chiba 288-0056, Japan.
Sakata
S
S
Kohgo
S
S
Matsuoka
M
M
Kodama
E
E
Mitsuya
H
H
Ohrui
H
H
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D015195:Drug Design; D006678:HIV / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008722:Methods; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D011684:Purine Nucleosides