Selective Action of 4?-Benzoylated Thymidine on DNA Polymerases and Reverse Transcriptases

Abstract

4?-Acylated thymidine triphosphates 1 have been synthesized and tested as substrates for DNA polymerases and reverse transcriptases. The 4?-benzoylated thymidine 1d was selectively acting as a chain terminator for the DNA synthesis catalyzed by retroviral RT. No incorporation of 1d was observed when DNA polymerases were used. The selective targeting of the action performed by retroviral enzymes is a requirement for an effective antiviral agent with a minimum of toxicity.