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131523

Novel Melatonin Derivatives: Synthesis, Anticancer Evaluations and Molecular-Docking Study

Article

Last updated: 01 Jan 2025

OverviewSimilar Items

Subjects

-

Tags

Organic chemistry

Abstract

Many studies mentioned that Melatonin considers an anti-cancer agent. So in this study, a lot of novel Melatonin derivatives incorporated different heterocyclic ring systems such as triazole, thiadiazole, tetrazole, thiazole, thiophene and pyrazole were synthesized. The synthesized compounds 5, 6, 8, 11, 15, 16 and 19 were evaluated as anti-cancer by using two human cancer cell lines, Breast cancer (MCF7) and colon cancer (HCT-116). The synthesized compounds showed a gradual decrease in the cell viability of the two cell lines. We also observed that compound 16 was the lowest IC50 and the highest cytotoxic effects against the two cancer cell lines. Furthermore, the molecular-docking study was employed to determine the possible mode of action of the synthesized compounds against proteins (CDK2 and P53-MDM2) which, were considered to be potential proteins involved in the pathogenesis of cancer. We observed that compound 16 was the best-docked ligand against the targeted proteins, as it displayed the lowest binding energies, critical hydrogen bonds, and hydrophobic interactions compared to other tested compounds.

DOI

10.21608/ejchem.2020.49430.3016

Keywords

Anticancer, azole, azine, THIOPHENE, Melatonin, molecular-docking

Authors

First Name

Mahmoud

Last Name

Alsayed

MiddleName

-

Affiliation

Department of Chemistry, Faculty of Science, Helwan University; Ain Helwan, Cairo 11795, A. R. Egypt

Email

m.a203050@yahoo.com

City

-

Orcid

-

First Name

Dina

Last Name

El-Kady

MiddleName

S.

Affiliation

Hormones Department, Medical Research Division, National Research Centre, Dokki, Giza, Egypt

Email

de.el-kady@nrc.sci.eg

City

-

Orcid

0000-0002-5809-5888

First Name

mohamed

Last Name

tantawy

MiddleName

A

Affiliation

Hormones Department, Medical Research Division, National Research Centre, Dokki, Giza, Egypt

Email

mohamed_tantawy@daad-alumni.de

City

CAIRO

Orcid

0000-0003-4014-6074

First Name

Mervat

Last Name

AbdElhalim

MiddleName

M.

Affiliation

Hormones Department, Medical Research Division, National Research Centre, Dokki, Giza, Egypt

Email

mm.abdelhalim@nrc.sci.eg

City

-

Orcid

0000-0002-6949-0744

First Name

Samia

Last Name

Elazabawy

MiddleName

R.

Affiliation

Department of Chemistry, Faculty of Science, Helwan University; Ain Helwan, Cairo 11795, A. R. Egypt

Email

samiaeradwan@science.helwan.edu.eg

City

-

Orcid

-

First Name

Amira

Last Name

Abdallah

MiddleName

E. M.

Affiliation

Ain Helwan

Email

amiraelsayed135@yahoo.com

City

Cairo

Orcid

0000-0002-6773-3634

First Name

Gamal

Last Name

Elmegeed

MiddleName

A

Affiliation

Hormones Department, Medical Research Division, National Research Centre, Dokki, Giza, Egypt

Email

ga.elmegeed@nrc.sci.eg

City

-

Orcid

0000-0003-1914-1543

Volume

64

Article Issue

3

Related Issue

21851

Issue Date

2021-03-01

Receive Date

2020-11-13

Publish Date

2021-03-01

Page Start

1,517

Page End

1,533

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 64_Issue 3_Pages 1517-1533.pdf

PDF . 1.2MB

Link

https://ejchem.journals.ekb.eg/article_131523.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=131523

Order

40

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Novel Melatonin Derivatives: Synthesis, Anticancer Evaluations and Molecular-Docking Study

Details

Type

Article

Created At

22 Jan 2023