ManageChatDiscover
377027

Design, Sequential Synthesis, Kinase Inhibitors Comparative Docking, MD Simulations, 99mTc-Coupling and In-Vivo Studies of Novel Pyrazolopyrimidine Derivatives

Article

Last updated: 27 Apr 2025

OverviewSimilar Items

Subjects

-

Tags

Pharmaceutical Chemistry

Abstract

Pyrazolopyrimidine derivative was synthesized and labeled with 99mTc using sodium dithionite as reducing agents. The purity of radiochemical 99mTc(Na2S2O4)-compound was 93.4%, and the synthesized complex was stable in vitro for 6 hours. Furthermore, using a radiolabeling technique, a bio-distribution investigation showed that tumor-bearing mice exhibited a remarkable absorption of [99mTc]Tc-complex, with a significant concentration in tumor tissues and a T/NT of 6.58 after 60 minutes after injection. These encouraging results mean that the synthesized compound offers a potential radio-carrier that can be used as a tumor marker and, following additional preclinical research, can be used for cancer therapy. Molecular dynamic simulation confirmed the stability of this compound in the active sites of both EGFR and VEGFR-2 receptors.

DOI

10.21608/ejchem.2024.302958.9979

Keywords

Pyrazolopyrimidines, Comparative docking, Kinase inhibitors, 99mTc-coupling, Tumor imaging, MD simulation

Authors

First Name

Wafaa

Last Name

Zaghary

MiddleName

Abdou

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Egypt.

Email

wafaa.zaghary@pharm.helwan.edu.eg

City

Cairo

Orcid

-

First Name

Dina

Last Name

Adel

MiddleName

-

Affiliation

Pharmaceutical Chemistry Department, Faculty of Pharmacy, MSA University, Cairo, Egypt

Email

dadel@msa.edu.eg

City

-

Orcid

-

First Name

basma

Last Name

Mohamed

MiddleName

-

Affiliation

Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, 13759, Cairo, Egypt

Email

basmamohamed24@yahoo.com

City

-

Orcid

-

First Name

Tamer

Last Name

Nasr

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Egypt

Email

tamerhefni@yahoo.com

City

-

Orcid

-

First Name

Khaled

Last Name

El-Adl

MiddleName

-

Affiliation

Heliopolis University

Email

eladlkhaled74@yahoo.com

City

Cairo

Orcid

0000-0002-8922-9770

First Name

tamer

Last Name

sakr

MiddleName

mostafa

Affiliation

Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, Cairo 13759, Egypt.

Email

tamer_sakr78@yahoo.com

City

-

Orcid

-

Volume

68

Article Issue

4

Related Issue

53790

Issue Date

2025-04-01

Receive Date

2024-07-09

Publish Date

2025-04-01

Page Start

271

Page End

284

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 68_Issue 4_Pages 271-284.pdf

PDF . 1.2MB

Link

https://ejchem.journals.ekb.eg/article_377027.html

Detail API

http://journals.ekb.eg?_action=service&article_code=377027

Order

377,027

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

https://ejchem.journals.ekb.eg/

MainTitle

Design, Sequential Synthesis, Kinase Inhibitors Comparative Docking, MD Simulations, 99mTc-Coupling and In-Vivo Studies of Novel Pyrazolopyrimidine Derivatives

Details

Type

Article

Created At

09 Apr 2025