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317258

Development of pyrazolo[1,5-a]pyrimidine derivatives: Synthesis, anticancer activity and docking study

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Last updated: 27 Dec 2024

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Abstract

It has been revealed that scaffolds made from pyrazolo[1,5-a]pyrimidines exhibit valuable biological activities, particulary anti-proliferative efficacy and blocking CDK kinase activity. Therefore, a new derivatives of Pyrazolo[1,5-a]pyrimidines 5a-c were synthesized, and their chemical structures were validated using several spectral studies. These compounds were screened against MCF-7, HCT-116, and HepG2 malignant cell lines in comparison to doxorubicin to determine their anticancer activity. From the results, it is found that the order of activity of the examined compounds in general is 5b with methoxy group which is better in activity than 5a having phenyl group and 5c bearing methyl group. The anti-tumor potency against HCT-116 demonstrated that compound 5b was promising and close to the reference (IC50 = 8.64 µM). In addition, the synthesized compounds were submitted to molecular docking research against CDK2 kinase enzyme in order to investigate the method of binding and understand the mechanism of the promising cytotoxic activity.

DOI

10.21608/aijpms.2023.203637.1207

Keywords

pyrazolo[1, 5-a]pyrimidines, Synthesis, Anticancer, docking simulation

Authors

First Name

Omneya

Last Name

Elbakry

MiddleName

M

Affiliation

Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt

Email

omneya_muhammad@azhar.edu.eg

City

-

Orcid

-

First Name

Marwa

Last Name

Harras

MiddleName

F

Affiliation

Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt

Email

marwaharras.pharmg@azhar.edu.eg

City

-

Orcid

-

First Name

Mohamed

Last Name

Elsebaei

MiddleName

M

Affiliation

Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt

Email

m.elsebaei@azhar.edu.eg

City

-

Orcid

0000-0002-0890-7219

First Name

Ahmed

Last Name

Mehany

MiddleName

B.M.

Affiliation

Department of Zoology, Faculty of Science(Boys), Al_azhar University, Cairo, Egypt

Email

abelal_81@yahoo.com

City

Nasr

Orcid

-

First Name

Hend

Last Name

Elsehrawi

MiddleName

-

Affiliation

Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt

Email

hendelsehrawi.pharmg@azhar.edu.eg

City

-

Orcid

-

Volume

4

Article Issue

1

Related Issue

44808

Issue Date

2024-01-01

Receive Date

2023-04-10

Publish Date

2024-01-01

Page Start

76

Page End

90

Print ISSN

2735-4598

Online ISSN

2735-4601

Article File

AIJPMS_Volume 4_Issue 1_Pages 76-90.pdf

PDF . 874.6kB

Link

https://aijpms.journals.ekb.eg/article_317258.html

Detail API

https://aijpms.journals.ekb.eg/service?article_code=317258

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Type

Original research articles

Type Code

1,562

Publication Type

Journal

Publication Title

Azhar International Journal of Pharmaceutical and Medical Sciences

Publication Link

https://aijpms.journals.ekb.eg/

MainTitle

Development of pyrazolo[1,5-a]pyrimidine derivatives: Synthesis, anticancer activity and docking study

Details

Type

Article

Created At

27 Dec 2024