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94135

Quinazolinone-Schiff's Base hybrids as Phosphodiesterase 4B inhibitors with dual activity against COPD and Lung Cancer

Article

Last updated: 01 Jan 2025

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Subjects

-

Tags

Pharmaceutical Chemistry

Abstract

A series of thirty compounds of quinazolinone-Schiff's base hybrids were rationally designed, synthesized, and evaluated for their in vitro Phosphodiesterase 4B inhibition, anti-lung and anti-colon cancer activities. Compounds 9, 16, 23, 29, 30, 31, 32 and 33, each possessing a tri-hydroxy moiety, showed the highest inhibitory activity (56.05-89.07%) at 10 µM concentration if compared to rolipram. Compounds 16 and 23 showed good anti-lung cancer activity with IC50 1.55 and 1.30 µM, respectively. Moreover, compound 16 showed high anti-colon cancer activity with IC50 0.6 µM. Compound 33 showed good affinity and molecular binding modes towards the key amino acid Gln 443 and Phe 446 for inhibition of the target enzyme. Finally, active compounds showed good ADME calculations.

DOI

10.21608/ejchem.2020.28992.2624

Keywords

Quinazolinone, Schiff's, Phosphodiesterase 4B, COPD, lung, Colon, Cancer

Authors

First Name

Mostafa

Last Name

Mansour

MiddleName

-

Affiliation

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University, Beni-Suef, Egypt

Email

mostafa.mansour@nub.edu.eg

City

-

Orcid

0000-0002-0179-8398

First Name

Mohammed

Last Name

El-Saadi

MiddleName

T

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt Medicinal Chemistry Department, Faculty of Pharmacy, Sinai University, Ismailia, Egypt.

Email

moh1_ttaha@yahoo.com

City

Beni-Suef

Orcid

-

First Name

Noha

Last Name

Amin

MiddleName

H

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt

Email

hani.noha@gmail.com

City

Beni-Suef

Orcid

-

First Name

Joshua

Last Name

Canzoneri

MiddleName

-

Affiliation

USA Mitchell Cancer Institute Drug Discovery Laboratory, University of South Alabama, USA.

Email

jcanzoneri@health.southalabama.edu

City

Mobile, Alabama, USA

Orcid

-

First Name

Adam

Last Name

Keeton

MiddleName

-

Affiliation

USA Mitchell Cancer Institute Drug Discovery Laboratory, University of South Alabama, USA.

Email

akeeton@health.southalabama.edu

City

Mobile, Alabama, USA

Orcid

-

First Name

Gary

Last Name

Piazza

MiddleName

-

Affiliation

USA Mitchell Cancer Institute Drug Discovery Laboratory, University of South Alabama, USA.

Email

gpiazza@health.southalabama.edu

City

Mobile, Alabama, USA

Orcid

-

First Name

hamdy

Last Name

abdelrahman

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Nahda University, Beni-suef, Egypt Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, 71526 Assiut, Egypt

Email

hamdy.abdelrahman@nub.edu.eg

City

assuit

Orcid

-

Volume

63

Article Issue

12

Related Issue

18901

Issue Date

2020-12-01

Receive Date

2020-04-29

Publish Date

2020-12-01

Page Start

4,851

Page End

4,866

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 63_Issue 12_Pages 4851-4866.pdf

PDF . 1.7MB

Link

https://ejchem.journals.ekb.eg/article_94135.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=94135

Order

17

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

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

MainTitle

Quinazolinone-Schiff's Base hybrids as Phosphodiesterase 4B inhibitors with dual activity against COPD and Lung Cancer

Details

Type

Article

Created At

22 Jan 2023