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

K Kitano; S Sakata; S Kohgo; M Matsuoka; E Kodama; H Mitsuya; H Ohrui

doi:10.1093/nass/44.1.105

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

Nucleic Acids Symp Ser. 2000:(44):105-6. doi: 10.1093/nass/44.1.105.

Authors

K Kitano¹, S Sakata, S Kohgo, M Matsuoka, E Kodama, H Mitsuya, H Ohrui

Affiliation

¹ Biochemicals Division, Yamasa Corporation, 2-10-1 Araoicho, Choshi, Chiba 288-0056, Japan.

PMID: 12903290
DOI: 10.1093/nass/44.1.105

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.

MeSH terms

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

Substances

Anti-HIV Agents
Purine Nucleosides