Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice

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, 1H and 13C NMR). The target compound was examined for its radioactivity and the results showed that benzo[g]quinazoline was successfully labeled with radioactive io...

Full description

Bibliographic Details
Main Authors: Rashad Al-Salahi, Moustapha E. Moustapha, Hatem A. Abuelizz, Abdulrahman I. Alharthi, Khalid A. Alburikan, Ismail T. Ibrahim, Mohamed Marzouk, Mohamed A. Motaleb
Format: Article
Language:English
Published: Elsevier 2018-12-01
Series:Saudi Pharmaceutical Journal
Online Access:http://www.sciencedirect.com/science/article/pii/S1319016418301257
id doaj-7dc16a5dde8f474583d590bc80a90732
record_format Article
spelling doaj-7dc16a5dde8f474583d590bc80a907322020-11-24T21:29:04ZengElsevierSaudi Pharmaceutical Journal1319-01642018-12-0126811201126Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing miceRashad Al-Salahi0Moustapha E. Moustapha1Hatem A. Abuelizz2Abdulrahman I. Alharthi3Khalid A. Alburikan4Ismail T. Ibrahim5Mohamed Marzouk6Mohamed A. Motaleb7Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Corresponding author.Department of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Al Kharj 11942, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Al Kharj 11942, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaLabeled Compound Department, Hot Laboratories Centre, Atomic Energy Authority, P.O. Box 13759, Cairo, EgyptDepartment of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Al Kharj 11942, Saudi Arabia; Chemistry of Natural Products Group, Center of Excellence for Advanced Sciences, National Research Centre, Dokki, Cairo 12622, EgyptLabeled Compound Department, Hot Laboratories Centre, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, 1H and 13C 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 125I-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. Keywords: Benzo[g]quinazoline, Radioiodination, Biodistribution, Tumor cell, NBShttp://www.sciencedirect.com/science/article/pii/S1319016418301257
collection DOAJ
language English
format Article
sources DOAJ
author Rashad Al-Salahi
Moustapha E. Moustapha
Hatem A. Abuelizz
Abdulrahman I. Alharthi
Khalid A. Alburikan
Ismail T. Ibrahim
Mohamed Marzouk
Mohamed A. Motaleb
spellingShingle Rashad Al-Salahi
Moustapha E. Moustapha
Hatem A. Abuelizz
Abdulrahman I. Alharthi
Khalid A. Alburikan
Ismail T. Ibrahim
Mohamed Marzouk
Mohamed A. Motaleb
Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice
Saudi Pharmaceutical Journal
author_facet Rashad Al-Salahi
Moustapha E. Moustapha
Hatem A. Abuelizz
Abdulrahman I. Alharthi
Khalid A. Alburikan
Ismail T. Ibrahim
Mohamed Marzouk
Mohamed A. Motaleb
author_sort Rashad Al-Salahi
title 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_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_sort radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3h)-one in tumor bearing mice
publisher Elsevier
series Saudi Pharmaceutical Journal
issn 1319-0164
publishDate 2018-12-01
description 3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, 1H and 13C 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 125I-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. Keywords: Benzo[g]quinazoline, Radioiodination, Biodistribution, Tumor cell, NBS
url http://www.sciencedirect.com/science/article/pii/S1319016418301257
work_keys_str_mv AT rashadalsalahi radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT moustaphaemoustapha radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT hatemaabuelizz radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT abdulrahmanialharthi radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT khalidaalburikan radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT ismailtibrahim radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT mohamedmarzouk radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
AT mohamedamotaleb radioiodinationandbiodistributionofnewlysynthesized3benzyl23methoxybenzylthiobenzogquinazolin43honeintumorbearingmice
_version_ 1725967608873746432

Similar Items