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196726

Design, synthesis, molecular docking and biological evaluation of novel 1,5-diarylpyrazole-N,O-dimethyl hydroxamate derivatives as antiproliferative agents.

Article

Last updated: 23 Dec 2024

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Subjects

-

Tags

Analytical and Medicinal Chemistry

Abstract

A series of novel hybrid of 1,5-diarylpyrazole-N,O-dimethylhydroxamate derivatives were designed and synthesised in synthetically acceptable yields. All the new synthesized compounds were biologically evaluated for their in vitro cytotoxicity against a panel of five cell lines namely human colorectal adenocarcinoma cell line DLD1, human cervical cancer cell line Hela, human leukemia cell line K562, human pancreatic cancer cell line Suit-2 and human hepatocellular carcinoma cell line HepG2. Compound 7a showed a significant cytotoxicity against Hela cell line with IC50 value of 16 µM and a good cytotoxicity against DLD1 and HepG2 with IC50 values of 69.9 µM and 78.8µM. Also, compound 7a displayed a potent EGFR inhibitory activity with IC50= 4.00 µM, which was comparable to positive reference drug sorafenib (IC50 = 3.5 µM). Moreover, in-silico studies showed that compound 7a has excellent binding affinity to the active site of EGFR with binding score better than a multitarget kinase drug sorafenib and good binding affinity to JNK-2, which explains the anticancer activity of compound 7a.

DOI

10.21608/jabps.2021.77469.1129

Keywords

pyrazole, hydroxamate, Cancer, eGFR

Authors

First Name

Heba

Last Name

Hassan

MiddleName

-

Affiliation

Med Chem Dept, Faculty of Pharmacy, Minia Uiversity

Email

heba.hasan@mu.edu.eg

City

-

Orcid

-

First Name

Kamal

Last Name

Abdelrahman

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut

Email

kamal_kamal20082002@yahoo.com

City

-

Orcid

-

First Name

Salah

Last Name

Abdel-aziz

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt

Email

salah72aa@yahoo.com

City

Assiut

Orcid

-

First Name

Adel

Last Name

Marzouk

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut

Email

adel_marzouk77@yahoo.com

City

-

Orcid

-

First Name

Hiroyuki

Last Name

Konno

MiddleName

-

Affiliation

Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Jonan 4-3-16, Yonezawa 992-8510, Japan

Email

konno@yz.yamagata-u.ac.jp

City

-

Orcid

konno@yz.yamagata-u.

First Name

Misato

Last Name

Tajiri

MiddleName

-

Affiliation

Department of Biochemical Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan

Email

ten28776@st.yamagata-u.ac.jp

City

-

Orcid

-

First Name

Mohamed

Last Name

Osman

MiddleName

-

Affiliation

Medicinal Chemistry Department, Faculty of Pharmacy, Minia University.

Email

abulnil@hotmail.com

City

Minia

Orcid

-

First Name

raef

Last Name

shams

MiddleName

-

Affiliation

Emergent Bioengineering Materials Research Team, RIKEN Centre for Emergent Matter Science, RIKEN, Wako, Saitama 351-0198, Japan.

Email

raef.shams@riken.jp

City

-

Orcid

-

Volume

4

Article Issue

4

Related Issue

27944

Issue Date

2021-10-01

Receive Date

2021-05-24

Publish Date

2021-10-01

Page Start

214

Page End

225

Print ISSN

2535-1869

Online ISSN

2535-2040

Article File

JABPS_Volume 4_Issue 4_Pages 214-225.pdf

PDF . 1.1MB

Link

https://jabps.journals.ekb.eg/article_196726.html

Detail API

https://jabps.journals.ekb.eg/service?article_code=196726

Order

3

Type

Original Article

Type Code

522

Publication Type

Journal

Publication Title

Journal of advanced Biomedical and Pharmaceutical Sciences

Publication Link

https://jabps.journals.ekb.eg/

MainTitle

Design, synthesis, molecular docking and biological evaluation of novel 1,5-diarylpyrazole-N,O-dimethyl hydroxamate derivatives as antiproliferative agents.

Details

Type

Article

Created At

22 Jan 2023