A novel 99mTc ‐diester complex as tumor targeting agent: synthesis, radiolabeling and biological distribution study

The target of this study is the synthesis of a new diester derivative and radiolabeling with one of the most effective diagnostic radioisotopes to be investigated as a novel targeting radiotracer for tumor imaging. 10 ‐[2‐(9‐carboxynonanoyloxy)propoxy]‐10‐oxodecanoic acid was synthesized in excellent yield and characterized by FT‐IR, mass,1HNMR and13C ‐NMR spectra. The diester was technetium‐99m radiolabeled by direct technique using sodium dithionite as a reducing agent. The labeling parameters such as diester amount, reducing agent amount, pH of the medium and reaction time were optimized. High radiochemical yield of 95.10 ± 0.41% and in‐ vitro stability in serum up to 12h have been obtained on complexation of the synthesized diester with Tc‐99m. Evaluation of the diester anticancer activity against breast cancer cell line (MCF‐7) showed high percent of inhibition about 61.5 % at 100 μg/ml. The rhenium complex of the diester was synthesized and characterized by LC‐MS (ESI) and elemental analysis depending on the strong chemical resemblance between Tc and Re. Biodistribution studies of99mTc ‐diester complex showed high target to non‐target ratio (T/NT) equals 6.24 ± 0.09 in tumor bearing mice at 30 min post injection, suggesting this complex could be used as hopeful solid tumor imaging agent.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research