CHEMISTRY AND ANTI-HIV ACTIVITY OF 2'-BETA-FLUORO-2',3'-DIDEOXYGUANOSINE

The 2'-beta-fluoro analogue of 2',3'-dideoxyguanosine has been prepare d by two synthetic routes. This compound and two analogues have anti-H IV activity in at least two of three host cell systems used (ATH8, CEM , PEL). These compounds, as well as their ddGuo parents, have been cha racterized with regard to their acid-stabilities, octanol-water partit ion coefficients, and enzyme substrate properties for adenosine deamin ase and purine nucleoside phosphorylase. F-ddGuo analogues are less po tent but more stable than their non-fluorinated parent compounds.