Synthesis of acyclothymidine triphosphate and α-P-boranotriphosphate and their substrate properties with retroviral reverse transcriptase
(Matrix presented) The first example of an acyclonucleoside α-P-boranotriphosphate has been synthesized via a phosphoramidite approach in a one-pot reaction with good yield. The presence of the α-P-BH3 in 5b results in a 9-fold increase in efficiency of incorporation by MMLV retroviral reverse transcriptase relative to non-boronated 5a in pre-steady-state conditions. The preliminary results indicate that acyclonucleoside α-P-boranotriphosphates may have promising applications as a probe of enzyme mechanisms and in the design of new antiviral drugs.
Li, Ping,Dobrikov, Mikhail,Liu, Hongyan,Shaw, Barbara Ramsay