PMID- 17434736
OWN - NLM
STAT- MEDLINE
DCOM- 20070830
LR  - 20191210
IS  - 0960-894X (Print)
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 17
IP  - 12
DP  - 2007 Jun 15
TI  - Synthesis and evaluation of 2'-substituted cyclobutyl nucleosides and nucleotides 
      as potential anti-HIV agents.
PG  - 3398-401
AB  - A series of 2'-substituted cyclobutyl nucleoside analogs were efficiently 
      prepared by constructing the core cyclobutyl ring using different [2+2] 
      cycloaddition approaches. The triphosphate derivative of a cyclobutyl nucleoside 
      was also synthesized and evaluated against wild-type and mutant HIV reverse 
      transcriptases (RT). Whereas the nucleoside analogs were inactive against HIV-1 
      in culture, the nucleotide showed good activity not only against wild-type and 
      recombinant HIV RT (IC(50)=4.7, 6.9 microM), but also against the M184I and M184V 
      mutants (IC(50)=6.1, 6.9 microM) in cell-free assays.
FAU - Li, Yongfeng
AU  - Li Y
AD  - Department of Chemistry, Emory University, Atlanta, GA 30322, USA.
FAU - Mao, Shuli
AU  - Mao S
FAU - Hager, Michael W
AU  - Hager MW
FAU - Becnel, Kimberlynne D
AU  - Becnel KD
FAU - Schinazi, Raymond F
AU  - Schinazi RF
FAU - Liotta, Dennis C
AU  - Liotta DC
LA  - eng
GR  - R37 AI028731/AI/NIAID NIH HHS/United States
GR  - 1R37AI-41890/AI/NIAID NIH HHS/United States
GR  - R01 AI028731/AI/NIAID NIH HHS/United States
GR  - 5P30-AI150409/AI/NIAID NIH HHS/United States
GR  - 2R37AI-28731/AI/NIAID NIH HHS/United States
PT  - Comparative Study
PT  - Evaluation Study
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, U.S. Gov't, Non-P.H.S.
DEP - 20070403
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Anti-HIV Agents)
RN  - 0 (Cyclobutanes)
RN  - 0 (Nucleosides)
RN  - 0 (Nucleotides)
RN  - 0 (Reverse Transcriptase Inhibitors)
SB  - IM
MH  - Anti-HIV Agents/chemical synthesis/*pharmacology
MH  - Binding Sites
MH  - Cells, Cultured
MH  - Cyclobutanes/*chemistry/pharmacology
MH  - Drug Resistance, Viral
MH  - Humans
MH  - Models, Chemical
MH  - Nucleosides/chemistry/*pharmacology
MH  - Nucleotides/chemistry/*pharmacology
MH  - Point Mutation
MH  - Reverse Transcriptase Inhibitors/chemical synthesis/*pharmacology
MH  - Structure-Activity Relationship
PMC - PMC5776709
MID - NIHMS25572
EDAT- 2007/04/17 09:00
MHDA- 2007/08/31 09:00
PMCR- 2018/01/22
CRDT- 2007/04/17 09:00
PHST- 2007/02/10 00:00 [received]
PHST- 2007/03/19 00:00 [revised]
PHST- 2007/03/29 00:00 [accepted]
PHST- 2007/04/17 09:00 [pubmed]
PHST- 2007/08/31 09:00 [medline]
PHST- 2007/04/17 09:00 [entrez]
PHST- 2018/01/22 00:00 [pmc-release]
AID - S0960-894X(07)00407-6 [pii]
AID - 10.1016/j.bmcl.2007.03.094 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2007 Jun 15;17(12):3398-401. doi: 
      10.1016/j.bmcl.2007.03.094. Epub 2007 Apr 3.