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64596

DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS

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Last updated: 25 Dec 2024

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Abstract

New designed EGFR inhibitors (7-11) were prepared from the pyrazolo[3,4-d]pyrimidine intermediates 4a-d including different moieties. All newly synthesized compounds were confirmed by elemental analyses and spectral data. The molecular simulation docking to protein tyrosine kinase (EGFR), using erlotinib (Tarceva TM) as a lead compound was also studied. Some of the prepared compounds were screened for in-vitro cytotoxic activity. The docking results were in coincidence with the biological results that indicated compound 7a showed an inhibitory activity against human breast carcinoma cell line (MCF-7) [IC50 (14.86μM)].

DOI

10.21608/bfsa.2012.64596

Authors

First Name

Rania

Last Name

Bakr

MiddleName

B.

Affiliation

Department of Pharmacutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt

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Orcid

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First Name

Eman

Last Name

Abdelall

MiddleName

K. A.

Affiliation

Department of Pharmacutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt

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Orcid

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First Name

Mohamed

Last Name

Abdel-Hamid

MiddleName

K.

Affiliation

Department of Organic Chemistry, Faculty of Pharmacy, Cairo University Cairo, Egypt

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City

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Orcid

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First Name

Manal

Last Name

Kandeel

MiddleName

M.

Affiliation

Department of Organic Chemistry, Faculty of Pharmacy, Cairo University Cairo, Egypt

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Volume

35

Article Issue

1

Related Issue

9673

Issue Date

2012-06-01

Receive Date

2012-01-24

Publish Date

2012-06-30

Page Start

27

Page End

42

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 35_Issue 1_Pages 27-42.pdf

PDF . 604.6kB

Link

https://bpsa.journals.ekb.eg/article_64596.html

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https://bpsa.journals.ekb.eg/service?article_code=64596

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Original Article

Type Code

1,096

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Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS

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Article

Created At

22 Jan 2023