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399756

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

Article

Last updated: 28 Dec 2024

OverviewSimilar Items

Subjects

-

Tags

Pharmaceutical Sciences

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.

DOI

10.21608/dusj.2024.267356.1053

Keywords

Monastrol, Quinolines, Dihydropyrimidin-2(1H)-one, Radioiodination, Tumor

Authors

First Name

Basem

Last Name

Mansour

MiddleName

-

Affiliation

Department 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.

Email

basem2412@yahoo.com

City

-

Orcid

0000-0001-6266-8864

First Name

mennatallah

Last Name

Sherif

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, Dakahlia, Egypt.

Email

mennatallahsherif0@gmail.com

City

Mansoura

Orcid

-

First Name

Ismail

Last Name

Ibrahim

MiddleName

T.

Affiliation

Labeled comp department, Hot lab center, Egyptian Atomic Energy Authority, Cairo 13759, Egypt.

Email

ismailtaha_73@yahoo.com

City

Cairo

Orcid

-

First Name

Magda

Last Name

El-Sayed

MiddleName

A.

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University, New Damietta, 34518, Egypt

Email

magdaaziz1@yahoo.com

City

Mansoura

Orcid

-

First Name

Mohammed

Last Name

Massoud

MiddleName

-

Affiliation

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt

Email

massoudmam@yahoo.fr

City

Mansoura

Orcid

-

First Name

Waleed

Last Name

Bayoumi

MiddleName

-

Affiliation

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt

Email

wabayoumi@gmail.com

City

Mansoura

Orcid

-

Volume

7

Article Issue

2

Related Issue

52436

Issue Date

2024-09-01

Receive Date

2024-02-02

Publish Date

2024-09-01

Page Start

40

Page End

51

Print ISSN

2636-3046

Online ISSN

2636-3054

Article File

DUSJ_Volume 7_Issue 2_Pages 40-51.pdf

PDF . 372.5kB

Link

https://dusj.journals.ekb.eg/article_399756.html

Detail API

https://dusj.journals.ekb.eg/service?article_code=399756

Order

399,756

Type

Original research papers

Type Code

1,769

Publication Type

Journal

Publication Title

Delta University Scientific Journal

Publication Link

https://dusj.journals.ekb.eg/

MainTitle

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

Details

Type

Article

Created At

28 Dec 2024