405238-78-0Relevant articles and documents
2′-fluoronucleosides
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, (2015/11/30)
2′-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base;R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy;R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; andR3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.
Structure-activity relationships of 2′-fluoro-2′,3′-unsaturated d-nucleosides as anti-hiv-1 agents
Lee, Kyeong,Choi, Yongseok,Gumina, Giuseppe,Zhou, Wen,Schinazi, Raymond F.,Chu, Chung K.
, p. 1313 - 1320 (2007/10/03)
We studied the structure-activity relationships of a series of 2′-fluoro-2′,3′-unsaturated D-nucleosides against HIV-1 in human peripheral blood mononuclear (PBM) cells. The target compounds 10-21 and 28-33 were prepared by N-glycosylation of the acetate
Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2',3'- unsaturated L-nucleosides
Lee, Kyeong,Choi, Yongseok,Gullen, Elizabeth,Schlueter-Wirtz, Susan,Schinazi, Raymond F.,Cheng, Yung-Chi,Chu, Chung K.
, p. 1320 - 1328 (2007/10/03)
The synthesis of L-nucleoside analogues containing 2'-vinylic fluoride was accomplished by direct condensation method, and their anti-HIV and anti- HBV activities were evaluated in vitro. The key intermediate 8, the sugar moiety of our target compounds, w
Synthesis and anti-HIV activity of L-2'-fluoro-2',3'-unsaturated purine nucleosides
Choi, Yongseok,Lee, Kyeong,Hong, Joon H.,Schinazi, Raymond F.,Chu, Chung K.
, p. 4437 - 4440 (2007/10/03)
The synthesis of 9-(2,3-dideoxy-2-fluoro-L-glycero-pent-2-eno- furanosyl)adenine and-hypoxanthine has been accomplished by direct condensation of silylated 6-chloropurine with key intermediates 8, which were prepared starting from 2,3-0-isopropylidene-L-glyceraldehyde. The synthesized nucleosides were evaluated against HIV-1 in vitro in primary human lymphocytes (PMB cells). It was found that β-L-Fd4A 12 exhibited moderately potent anti-HIV activity (EC50 1.5 μM).
