1571988-89-0Relevant articles and documents
Synthesis and antiviral evaluation of novel 2′,2′-difluoro 5′-norcarbocyclic phosphonic acid nucleosides as antiviral agents
Shen, Guang Huan,Hong, Joon Hee
, p. 1 - 17 (2014/03/21)
A very efficient synthetic route to novel 2′,2′-difluoro 5′-norcarbocyclic phosphonic acid nucleosides from but-3-en-1-ol 5 is described. The discovery of 2′-fluorinated furanose nucleoside 1 as a potent anti-HIV-1 agent has led to the synthesis and biological evaluation of 2′-modified 5′-norversions of the carbocyclic phosphonate nucleosides. The synthesized nucleoside analogues 18, 19, 23a, 23b, and 24 were tested for anti-HIV activity as well as cytotoxicity. Adenine analogue 19 shows significant anti-HIV-1 activity (EC50 = 13 μM).
