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AZT 5'-Cholinephosphate as an anti-HIV agent: the study of biochemical properties and metabolic transformations using
Dmitry V Yanvarev1, Elena A Shirokova, Maria V Astapova
1Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, Russian Federation. vsupport@bk.ru
Abstract:
Biochemical and metabolic transformations of 3'-azido-3'-deoxythymidine 5'-choline phosphate (1) were studied using its 32P-labelled counterpart for the evaluation of possible reasons for its enhanced anti-HIV activity. An effective synthesis of 32P-labelled 1 with a specific activity >1,000 Ci/mmol was developed by esterification of 32P-phosphoric acid with choline in the presence of BrCN followed by the coupling of the resulting choline phosphate with 3'-azido-3'-deoxythymidine (AZT). Chemical and enzymatic stabilities of 1 as well as the dynamics of penetration through HL-60 cell membranes were studied at the concentrations comparable to its antiviral concentrations. The products of intracellular transformations of the studied nucleotide were identified.
