1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging
Mansour, B., Sherif, M., Ibrahim, I., El-Sayed, M., Massoud, M., Bayoumi, W. (2024). 1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging. EKB Journal Management System, 7(2), 40-51. doi: 10.21608/dusj.2024.267356.1053
Basem Mansour; mennatallah Sherif; Ismail T. Ibrahim; Magda A. El-Sayed; Mohammed Massoud; Waleed Bayoumi. "1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging". EKB Journal Management System, 7, 2, 2024, 40-51. doi: 10.21608/dusj.2024.267356.1053
Mansour, B., Sherif, M., Ibrahim, I., El-Sayed, M., Massoud, M., Bayoumi, W. (2024). '1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging', EKB Journal Management System, 7(2), pp. 40-51. doi: 10.21608/dusj.2024.267356.1053
Mansour, B., Sherif, M., Ibrahim, I., El-Sayed, M., Massoud, M., Bayoumi, W. 1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging. EKB Journal Management System, 2024; 7(2): 40-51. doi: 10.21608/dusj.2024.267356.1053

1,2,3,4-Tetrahydropyrimidine-clubbed quinoline hybrid: Radiolabeling, Biodistribution and Imaging

Delta University Scientific Journal
Volume 7, Issue 2, September 2024, Page 40-51  XML PDF (363.81 K)
Document Type: Original research papers
DOI: 10.21608/dusj.2024.267356.1053
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Authors
Basem Mansour email orcid 1; mennatallah Sherif2; Ismail T. Ibrahim3; Magda A. El-Sayed4; Mohammed Massoud5; Waleed Bayoumi5
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, Dakahlia, Egypt. Department of pharmaceutical chemistry, Kut University College, Al Kut, Wasit 52001 Iraq.
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, Dakahlia, Egypt.
3Labeled comp department, Hot lab center, Egyptian Atomic Energy Authority, Cairo 13759, Egypt.
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt
5Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Abstract
Cancer represents a broad category encompassing various diseases that can impact any area of the body. It is also referred to as malignant tumors or neoplasms. Aiming to diagnose tumors, a promising monastrol analogue (1b) methyl 4-(2-hydroxyquinolin-3-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate, was designed via structural modification of monastrol, and synthesized in good yield. This compound was in vitro evaluated via MTT assay and revealed potent antitumor effects on a panel of cancer cell lines namely; HepG-2, HCT-116, MCF-7, and PC3 against standard 5-fluorouracil. The target 1b was radiolabeled with iodine-131 by a direct electrophilic substitution reaction. It was found that 131I-1b has a high radiolabeling yield (96.40 ± 2.00%), stability, solid tumor uptake, and Target/Non-target ratio (T/NT) ratio (5 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.
Keywords
Monastrol; Quinolines; Dihydropyrimidin-2(1H)-one; Radioiodination; Tumor
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