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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...

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Autores principales: Al-Salahi, Rashad, Moustapha, Moustapha E., Abuelizz, Hatem A., Alharthi, Abdulrahman I., Alburikan, Khalid A., Ibrahim, Ismail T., Marzouk, Mohamed, Motaleb, Mohamed A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2018
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.
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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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