EVALUATION OF 2-(3-AMINOBENZAMIDO)-2-DEOXY-D-GLUCOSE AS A RADIOSENSITIZER

PURPOSE: 3-Aminobenzamide (3-AB), an inhibitor of poly(adenosine dipho sphate [ADP]-ribose) synthetase, functions as a radiosensitizer in sev eral human tumor cell lines. 2-(3-AB)-2-deoxy-D-glucose (3-AB-G) was d esigned to increase preferentially the intracellular concentration of the drug in tumor cells. Both the toxicity and effectiveness of 3-AB-G as a radiosensitizer were determined. MATERIALS AND METHODS: The toxi city of 3-AB-G was measured in HeLa and Chinese hamster ovary cells. T he radiosensitizing effect of 3-AB-G was determined for both cell line s. RESULTS: 3-AB-G was not toxic to cells at concentrations of 10 mmol /L or less. 3-AB-G did not alter cell survival after irradiation. CONC LUSION: 3-AB-G was not an effective radiosensitizer for the cells test ed. Coupling 2-deoxyglucose to 3-AB may block the uptake of the inhibi tor into the cell by altering the ability of the receptor to recognize the molecule or may interfere with the specificity of the inhibitor f or poly(ADP-ribose) synthetase.