title: Development and bioevaluation of 99mTc(CO)3-labeled (1-azido-1-deoxy-β-D-glucopyranoside) complex as a potential tumor-seeking agent.
abstract: The 1,2,3-triazole-containing (1-azido-1-deoxy-β-D-glucopyranoside) complex was synthesized using click chemistry approach and evaluated its potential as a tumor-seeking agent. In the present study, (99m)Tc-tricarbonyl labeled (1-azido-1-deoxy-β-D-glucopyranoside) radiotracer [(99m)Tc(CO)(3)-BM], (where BM stands for biomolecule, e.g., (1-azido-1-deoxy-β-D- glucopyranoside)) was synthesized via click chemistry approach and then labeled with technetium-99m through isolink kit. Radio labeled drug was tested for radiochemical purity and in vitro stability by chromatographic techniques. Normal distribution and tumoral uptake were studied in Swiss Webster mice. Radiochemical purity results show 97.9 ±1.5% labeling and its in vitro stability were studied at room temperature up to 5h. The radio labeled drug exhibited 73.6±1.1% binding with blood proteins. Normal distribution of drug shows prominent uptake in brain while in case of tumor-bearing mice, the uptake was maximum in tumor tissue and negligible amount was shown in brain. The biodistribution was further compared with 2-fluoro-2-deoxy glucose ((18)F-FDG), which was used as a positive control. The data indicate that (99m)Tc-tricarbonyl labeled (1-azido-1-deoxy-β-D- glucopyranoside) radiotracer might be a feasible candidate with reasonable potential for tumor diagnosis.
authors.affiliation: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine and Oncology (INMOL), Lahore, Pakistan.
authors.forename: IrfanUllah
authors.initials: I
authors.lastname: Khan
authors.affiliation: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine and Oncology (INMOL), Lahore, Pakistan.
authors.forename: Abubaker
authors.initials: A
authors.lastname: Shahid
authors.affiliation: Institute of Chemistry, University of the Punjab, Quaid-e-Azam Campus, Lahore, Pakistan.
authors.forename: Ume Kalsoom
authors.initials: UK
authors.lastname: Dar
authors.affiliation: Radiopharmacy and PET Radiochemistry Division, Institute of Nuclear Medicine and Oncology (INMOL), Lahore, Pakistan.
authors.forename: Fayyaz
authors.initials: F
authors.lastname: Ahmad
authors.affiliation: Gujranwala Institute of Nuclear Medicine (GINUM), Nizampur, Sialkot Road, Gujranwala, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Javed
mesh_terms: D000818:Animals; D004355:Drug Stability; D007553:Isotope Labeling; D051379:Mice; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging*; D011485:Protein Binding; D011786:Quality Control; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals; D013667:Technetium; D014018:Tissue Distribution
chemical_list: D019275:Radiopharmaceuticals; D013667:Technetium