Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine.
Asymmetric synthesis of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine and its analogs were accomplished and their anti-HIV activities were evaluated. It was found that L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine exhibited moderately potent anti-HIV (EC50 = 2.4 microM) activity in human PBM cells without cytotoxicity up to 100 microM.
Wang
P
P
Center for Drug Discovery, University of Georgia College of Pharmacy, Athenes, GA 30602, USA.
Schinazi
R F
RF
Chu
C K
CK
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D002522:Chlorocebus aethiops; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D014709:Vero Cells
D019380:Anti-HIV Agents; C116654:carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine; D000241:Adenosine