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283708

Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition

Article

Last updated: 01 Jan 2025

OverviewSimilar Items

Subjects

-

Tags

Pharmaceutical Chemistry

Abstract

Depriving the estrogen in the body by inhibiting the aromatase enzyme is thought to be one of the most effective pathways for preventing and treating breast cancer. This study deals with the synthesis of new derivatives bearing a 4-bromophenyl-5-methyl-1,2,3-triazole scaffold hybridized with various heterocyclic rings of reported aromatase inhibition activity such as pyridine, pyrimidine, and pyrazole 4-14, aiming to gain new potent antiproliferative molecules against breast cancer via inhibition of the aromatase enzyme. The cytotoxic activity of the target compounds was evaluated against breast cancer (MCF-7) as well as the normal cell line (WI-38). The derivatives 5b, 5c and 10 were the most promising analogues with a high safety margin against WI38. The latter derivatives were also assessed as aromatase inhibitors and were also subjected to molecular docking studies to determine their potential.

DOI

10.21608/ejchem.2023.179241.7278

Keywords

1, 2, 3-Triazole, breast cancer, Aromatase Inhibitors, Molecular docking, Cytotoxicity

Authors

First Name

Yasmin M.

Last Name

Syam

MiddleName

-

Affiliation

Department of Therapeutic Chemistry, National Research Centre, Dokki, Cairo, Egypt

Email

yasminsyam24@gmail.com

City

-

Orcid

-

First Name

Radwan

Last Name

EL-Hggar

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt.

Email

radwan_elhaggar@pharm.helwan.edu.eg

City

-

Orcid

0000-0002-3878-9890

First Name

Manal

Last Name

Anwar

MiddleName

M.

Affiliation

Therapeutic Chemistry Department, National Research Centre, Cairo, Egypt.

Email

manalhassan232@ymail.com

City

-

Orcid

-

First Name

Alaa H.

Last Name

Hisham

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt.

Email

dr.alaa.hesham93@gmail.com

City

-

Orcid

-

First Name

Ola

Last Name

Nosseir

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt

Email

ola.nosseir@pharm.helwan.edu.eg

City

-

Orcid

-

First Name

Wafaa A.

Last Name

Zaghary

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, P.O. Box 11795, Cairo, Egypt

Email

wzaghary@yahoo.com

City

-

Orcid

-

Volume

66

Article Issue

10

Related Issue

43169

Issue Date

2023-10-01

Receive Date

2022-12-07

Publish Date

2023-10-01

Page Start

93

Page End

106

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 66_Issue 10_Pages 93-106.pdf

PDF . 608.7kB

Link

https://ejchem.journals.ekb.eg/article_283708.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=283708

Order

283,708

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition

Details

Type

Article

Created At

30 Dec 2024