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Abstract
In this thesis, the labeling of Thioguanine as a member of antimetabolites family was carried out by direct iodination of Thioguanine (100g) with radioiodine in a fast single step at 60ºC, to produce iodo-6-Thioguanine(125I-S6G). Chloramine-T (200g) was used as oxidizing agent at pH 7 and the reaction time was 30 min. A high radiochemical yield of 96.4% was obtained. The biodistribution of 125I-6-thioganine was studied in both normal and tumor bearing mice. The uptake in ascetic fluid was 35.4% and 23.9% at 1 and 24 hours post intravenous injection (h.p.i.), respectively, indicating the suitability of this labeled compound to be used as a radiopharmaceutical agent.
Also, in this thesis the labeling of Melphalan which is a member of alkylating agent’s family with radioactive iodine-125 was done. The optimum conditions of the labeling of Melphalan to give a radiochemical yield of 96.8 % were 200 g Melphalan, 150 l of Chloramine-T (150 g) and 150 l phosphate buffer pH 7 when the reaction mixture was heated at 70oC for 15 min.. The biodistribution of 125I-Melphalan was studied in both normal and tumor bearing mice. All the obtained data demonstrate that, the tracer was distributed rapidly through out the body after intravenous injection (2 hours,) and cleared through the hepatobiliary system (24 hours). In addition, the bio-distribution of the tracer in tumor bearing
mice demonstrated the possibility of the use of this tracer as imaging or therapeutic agent for cancer.