[Conformation of crystalline 3'-nitro-2',3'-dideoxythymidine and properties of its 5'-triphosphate as a terminator substrate of retroviral reverse transcriptase]. / Konformatsiia 3'-nitro-2',3'-didezoksitimidina v kristalle i svoistva ego 5'-trifosfata kak terminatornogo substrata obratnykh transkriptaz retrovirusov.

The structure of new nucleoside--3'-nitro-2',3'-dideoxythymidine (NIT) possessing moderate anti HIV activity in MT-4 cell culture was investigated by X-ray analysis. These data showed that conformation of NIT in crystal is similar to that of one of crystallographically independent forms of 3'-azido-2',3'-dideoxythymidine. 3'-Nitro-2',3'-dideoxythymidine 5'-triphosphate (NITTP) was synthesized and its ability to inhibit human and viral DNA polymerases was studied. NITTP proved to be effective and highly selective terminating substrate of DNA synthesis catalyzed by HIV and AMV reverse transcriptases. Human DNA polymerase alpha as well as DNA polymerase beta (rat liver), terminal deoxynucleotidyltransferase (calf thymus) or HSV-1 and CMV DNA polymerases did not incorporate NITTP into a growing DNA chain.