Synthesis, antitumor evaluation and labeling of N-(p-Tolyl)‎-2, 4 azepandione with 99mTc as a tumor imaging agent

Abstract EN

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 1mg AZD, 3mg ethylenediamine tetraacetic acid (EDTA) and 50^g/10^l stannous chloride at room temperature within 15min 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.