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Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice
3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, (1)H and (13)C NMR). The target compound was examined for its radioactivity and the results showed that benzo[g]quinazoline was successfully labeled with radioactiv...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6260473/ https://www.ncbi.nlm.nih.gov/pubmed/30532632 http://dx.doi.org/10.1016/j.jsps.2018.06.001 |
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author | Al-Salahi, Rashad Moustapha, Moustapha E. Abuelizz, Hatem A. Alharthi, Abdulrahman I. Alburikan, Khalid A. Ibrahim, Ismail T. Marzouk, Mohamed Motaleb, Mohamed A. |
author_facet | Al-Salahi, Rashad Moustapha, Moustapha E. Abuelizz, Hatem A. Alharthi, Abdulrahman I. Alburikan, Khalid A. Ibrahim, Ismail T. Marzouk, Mohamed Motaleb, Mohamed A. |
author_sort | Al-Salahi, Rashad |
collection | PubMed |
description | 3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, (1)H and (13)C NMR). The target compound was examined for its radioactivity and the results showed that benzo[g]quinazoline was successfully labeled with radioactive iodine using NBS via an electrophilic substitution reaction. The reaction parameters that affected the labeling yield such as concentration, pH and time were studied to optimize the labeling conditions. The radiochemical yield was 91.2 ± 1.22% and the in vitro studies showed that the target compound was stable for up to 24 h. The thyroid was among the other organs in which the uptake of (125)I-benzoquinazoline has increased significantly over the time up to 4.1%. The tumor uptake was 6.95%. Radiochemical and metabolic stability of the benzoquinazoline in vivo/in vitro and biodistribution studies provide some insights about the requirements for developing more potent radiopharmaceutical for targeting the tumor cells. |
format | Online Article Text |
id | pubmed-6260473 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-62604732018-12-07 Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice Al-Salahi, Rashad Moustapha, Moustapha E. Abuelizz, Hatem A. Alharthi, Abdulrahman I. Alburikan, Khalid A. Ibrahim, Ismail T. Marzouk, Mohamed Motaleb, Mohamed A. Saudi Pharm J Article 3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, (1)H and (13)C NMR). The target compound was examined for its radioactivity and the results showed that benzo[g]quinazoline was successfully labeled with radioactive iodine using NBS via an electrophilic substitution reaction. The reaction parameters that affected the labeling yield such as concentration, pH and time were studied to optimize the labeling conditions. The radiochemical yield was 91.2 ± 1.22% and the in vitro studies showed that the target compound was stable for up to 24 h. The thyroid was among the other organs in which the uptake of (125)I-benzoquinazoline has increased significantly over the time up to 4.1%. The tumor uptake was 6.95%. Radiochemical and metabolic stability of the benzoquinazoline in vivo/in vitro and biodistribution studies provide some insights about the requirements for developing more potent radiopharmaceutical for targeting the tumor cells. Elsevier 2018-12 2018-06-06 /pmc/articles/PMC6260473/ /pubmed/30532632 http://dx.doi.org/10.1016/j.jsps.2018.06.001 Text en © 2018 The Authors http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Article Al-Salahi, Rashad Moustapha, Moustapha E. Abuelizz, Hatem A. Alharthi, Abdulrahman I. Alburikan, Khalid A. Ibrahim, Ismail T. Marzouk, Mohamed Motaleb, Mohamed A. Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title | Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title_full | Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title_fullStr | Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title_full_unstemmed | Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title_short | Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice |
title_sort | radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3h)-one in tumor bearing mice |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6260473/ https://www.ncbi.nlm.nih.gov/pubmed/30532632 http://dx.doi.org/10.1016/j.jsps.2018.06.001 |
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