Synthesis, antitumor evaluation labeling of N-(p-Tolyl)-2,4- azepandione with 9\'9mTc as a tumor imaging agent

The compound N-(p-Tolyl) -2,4-Azepandione (AZD) was synthesized and characterized with different analytical techniques. The cytotoxic (antitumor) effect was estimated on MCF-7 human cell line. It showed a significant and encouragement effect as cytotoxic agent. The cytotoxic effect of AZD was increased with the increase of its dose. Labeling of AZD with 99mTc was performed at ph 6 using 1 mg AZD, 3 mg ethylenediamine tetraacetic acid (EDTA) and 50μg/10μl stannous chloride at room temperature within 15 min reaction time.The radiochemical yield of 99mTc-AZD was 95% as estimated by paper chromatography and electrophoresis. Biodistribution of 99mTc-AZD in tumor bearing mice showed that it is oriented towards tumor sites with higher percent than the other antitumor agents. The uptake of 99mTc-AZD in both ascites and solid tumor may be sufficient to radio image tumor sites. AZD may be considered as a promising antitumor agent as well as a tumor imaging agent upon labeling with technetium-99m