RADIOIODINATED 2-NITROBENZYL CARBAMATES AS BIOREDUCTIVE ALKYLATING-AGENTS FOR TISSUE HYPOXIA

Three N-methylcarbamates of iodonitrobenzyl alcohols (4-iodo-2-nitrobe nzyl alcohol 2, 5-iodo-2-nitrobenzyl alcohol 3 and 4-iodo-2,6-dinitrob enzyl alcohol 4) bearing [I-125] have been prepared and characterized for their lipophilicity, their reduction potentials and the in vivo la bility of the radioiodine in healthy mice. Based upon these results, 2 and 4 were tested in tumour-bearing mice showing limited uptake of ra dioactivity in tumours and a tumour-to-blood ratio of less than 1. Con sequently these particular carbamates are not satisfactory as hypoxia imaging agents.