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Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity

Article

Last updated: 01 Jan 2025

OverviewSimilar Items

Subjects

-

Tags

Organic chemistry

Abstract

A series of Nα-phthaloyl bridged cyclic pentapeptide derivatives were synthesized and characterized on the basis of spectral and elemental analyses. A preliminary cytotoxicity evaluation of all novel compounds was carried out against four human cancer cell lines, human lung (A-549), colon (CaCo-2), prostate (PC-3) and breast (MCF-7) cancer cells at 100 μM concentration using MTT growth inhibition assay. Compound 3 gave the highest cytotoxic activity towards the human colon (CaCo-2) cancer cell line (Growth Inhibition = 72.4 %). Further molecular docking of the promising derivative 3 was developed to study its binding mode within the active site of EGFR enzyme. The docking results suggest good fitting through different hydrogen bond interactions with the protein residues to elicit anticancer activity

DOI

10.21608/ejchem.2019.18452.2137

Keywords

amino acid, linear peptide, cyclic pentapeptide, Nα-phthaloyl-bis-peptides, Cytotoxicity

Authors

First Name

Fatma

Last Name

Mohamed

MiddleName

Hassan

Affiliation

Peptide Chemistry Department, National Research Centre, Dokki 12622, Cairo, Egypt

Email

fatmahassan1581993@gmail.com

City

Geza

Orcid

-

First Name

Ahmed

Last Name

Shalaby

MiddleName

-

Affiliation

Peptide Chemistry Department, Chemical Industries Research Division, National Research Centre, Cairo, Egypt

Email

ahshalaby45@gmail.com

City

Geza

Orcid

-

First Name

Hanan

Last Name

Soliman

MiddleName

abdelhameid

Affiliation

Biochemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt

Email

hanan_abdelhameid@yahoo.com

City

-

Orcid

-

First Name

Ahmed

Last Name

Abdelazem

MiddleName

-

Affiliation

Biotechnology and Life Sciences Department, Faculty of Postgraduate Studies for Advanced Sciences, Beni-Suef University, Egypt

Email

aznagi2003@gmail.com

City

-

Orcid

-

First Name

Marwa

Last Name

Mounier

MiddleName

-

Affiliation

Pharmaceutical and Drug Industries Research Division, Department of Pharmacognosy, National Research Centre, Giza, Egypt

Email

marwa_m3@yahoo.com

City

-

Orcid

-

First Name

Eman

Last Name

Nossier

MiddleName

-

Affiliation

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

Email

dremannossier@azhar.edu.eg

City

-

Orcid

0000-0001-6159-5333

First Name

Gaber

Last Name

Moustafa

MiddleName

-

Affiliation

Peptide Chemistry Department, National Research Centre, Dokki 12622, Cairo, Egypt

Email

gosman79@gmail.com

City

Geza

Orcid

-

Volume

63

Article Issue

5

Related Issue

10591

Issue Date

2020-05-01

Receive Date

2019-10-20

Publish Date

2020-05-01

Page Start

1,723

Page End

1,736

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 63_Issue 5_Pages 1723-1736.pdf

PDF . 1.7MB

Link

https://ejchem.journals.ekb.eg/article_58172.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=58172

Order

10

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity

Details

Type

Article

Created At

22 Jan 2023