Peer-Reviewed Journal Details
Mandatory Fields
Debarge, S,Balzarini, J,Maguire, AR;
2011
January
The Journal of Organic Chemistry
Design and Synthesis of alpha-Carboxy Phosphononucleosides
Validated
()
Optional Fields
H INSERTION REACTIONS ANTI-HIV ACTIVITY ACYCLIC NUCLEOSIDE PHOSPHONATES CARBENOID MEDIATED CYCLIZATIONS TERT-BUTYLDIMETHYLSILYL GROUP OF-THE-ART REVERSE-TRANSCRIPTASE BIOLOGICAL-ACTIVITY DNA-POLYMERASES CYCLIC ETHERS
76
105
126
Rhodium catalyzed O-H insertion reactions employing alpha-diazophosphonate 20 with appropriately protected thymidine, uridine, cytosine, adenosine and guanosine derivatives leads to novel 5'-phosphononucleoside derivatives. Deprotection led to a novel series of phosphono derivatives bearing a carboxylic acid moiety adjacent to the phosphonate group with potential antiviral and/or anticancer activity. The phosphononucleosides bearing an alpha-carboxylic acid group are envisaged as potential diphosphate mimics. Conversion to mono- and diphosphorylated phosphononucleosides has been effected for evaluation as nucleoside triphosphate mimics. Most of the novel phosphononucleosides proved to be inactive against a variety of DNA and RNA viruses. Only the phosphono AZT derivatives 56-59 showed weak activity against HIV-1 and HIV-2.
DOI 10.1021/jo101738e
Grant Details