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Reverse Transcriptase

AZT 5'-triphosphate mimics inhibit HIV reverse transcriptase

Published in AIDS Weekly, March 21st, 2005

AZT 5'-triphosphate mimics inhibit HIV reverse transcriptase.

According to recent research published in the Journal of Medicinal Chemistry, "In search of active nucleoside 5'-triphosphate mimics, we have synthesized a series of AZT triphosphate mimics (AZT P3Ms) and evaluated their inhibitory effects on HIV-1 reverse transcriptase as well as their stability in fetal calf serum and in CEM cell extracts."

"Reaction of AZT with 2-chloro-4H-1,3,2-benzodioxaphosphorin-4-one, followed by treatment of the phosphite intermediate 2 with pyrophosphate analogues, yielded the cyclic triphosphate intermediates 4b-4f, which were subjected to boronation and...

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