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

被引：12

作者：

Al-Salahi, Rashad ^{[1
]}

Moustapha, Moustapha E. ^{[2
]}

Abuelizz, Hatem A. ^{[1
]}

Alharthi, Abdulrahman, I ^{[2
]}

Alburikan, Khalid A. ^{[3
]}

Ibrahim, Ismail T. ^{[4
]}

Marzouk, Mohamed ^{[2
,5
]}

Motaleb, Mohamed A. ^{[4
]}

机构：

[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, POB 2457, Riyadh 11451, Saudi Arabia

[2] Prince Sattam Bin Abdulaziz Univ, Coll Sci & Humanities, Dept Chem, POB 83, Al Kharj 11942, Saudi Arabia

[3] King Saud Univ, Coll Pharm, Dept Clin Pharm, POB 2457, Riyadh 11451, Saudi Arabia

[4] Atom Energy Author, Hot Labs Ctr, Labeled Compound Dept, POB 13759, Cairo, Egypt

[5] Natl Res Ctr, Ctr Excellence Adv Sci, Chem Nat Prod Grp, Cairo 12622, Egypt

来源：

SAUDI PHARMACEUTICAL JOURNAL | 2018年 / 26卷 / 08期

关键词：

Benzo[g]quinazoline; Radioiodination; Biodistribution; Tumor cell; NBS; THERAPY; AGENT;

D O I：

10.1016/j.jsps.2018.06.001

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, H-1 and C-13 NMR). The target compound was examined for its radioactivity and the results showed that benzo[glquinazoline 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 I-123-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. (C) 2018 The Authors. Production and hosting by Elsevier B.V.

引用

页码：1120 / 1126

页数：7

共 32 条

[1] 3-Benzyl(phenethyl)-2-thioxobenzo[g]quinazolines as a new class of potent α-glucosidase inhibitors: synthesis and molecular docking study [J].