Abstract
New conjugated arylidine, enamine, and annelated pyrido derivatives of quinoxaline 1,4-dioxide were synthesized via utilization of an active allylic methyl group. Biodistribution studies were carried out by injecting a solution of an 125I derivative of an enamine-substituted quinoxaline 1,4-dioxide in normal and tumor-bearing mice. The uptake in solid tumor was over 6% of the injected dose per gram tissue body weight at 4 h post injection. These data revealed localization of the tracer in the tumor tissues with a high percentage sufficient to show a radiotherapeutic effect and showed that this is a promising tool for diagnosis. Also the radiotoxicity of the 125I-substituted compound on Ehrlich ascites carcinoma cells may encourage this behavior.
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