COMPARISON OF THE DNA INCORPORATION IN HUMAN MOLT-4 CELLS OF 2 2'-BETA-FLUORONUCLEOSIDES, 2'-BETA-FLUORO-2',3'-DIDEOXYADENOSINE AND FIALURIDINE

Incorporation of 2'-beta-fluoro-2',3'-dideoxyadenosine (F-ddA), a rece ntly developed anti-HIV agent, into the cellular DNA of human MOLT-4 c ells has been compared with the DNA incorporation seen with fialuridin e (FIAU; -2'-fluoro-beta-D-arabinofuranosyl]-5-iodouracil), a potent a nti-hepatitis B (anti-HBV) nucleoside analogue recently found to cause severe hepatic toxicity in human subjects. At equimolar concentration s (10 mu M), incorporation of F-ddA was less than 1% of that for FIAU, a difference attributable to the lack of a 3'-hydroxyl group in the f ormer compound and a consequent inability of F-ddA, unlike FIAU, to fo rm DNA internucleotide linkages.