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239431

SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES

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Last updated: 04 Jan 2025

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Abstract

Two novel derivatives of cyclosporin A were designed and synthesized. Synthesis of target compounds has been performed using olefin metathesis chemistry. The structures of target compounds were confirmed using 1H and 13C NMR and high-resolution mass spectroscopy. The in vitro antiproliferative effect of the two compounds was tested over NCI-60 cancer cell lines of nine different cancer types. The piperidinedione derivative (compound 7) had an inhibitory effect higher than 80% over 13 cancer cell lines, and close to or higher than 100% over six cancer cell lines. Compound 7 showed also significantly higher inhibitory activity than cyclosporin A against non-small cell lung cancer NCI-H226 cell line. Moreover, compound 7 showed an overall moderate antiproliferative activity against the NCI-60 cancer cell lines with a mean value of 57.54 %. While, the pyrrolidindione derivative (compound 6) showed weak antiproliferative activity against the NCI-60 cancer cell lines with a mean value of 28.83%. Finally, the predicted pharmacokinetic properties of compounds 6 and 7 were better than that of cyclosporine A.

DOI

10.21608/bfsa.2022.239431

Keywords

Synthesis, Anti-proliferative effect, Cyclosporin A, olefin metathesis, pharmacokinetic

Authors

First Name

Ahmed

Last Name

Abdelazem

MiddleName

Z.

Affiliation

Biotechnology & Life Sciences Department, Faculty of Postgraduate Studies for Advanced Sciences, Beni-Suef University, Beni-Suef 62517, Egypt

Email

aznagi@psas.bsu.edu.eg

City

-

Orcid

https://orcid.org/00

First Name

So

Last Name

Lee

MiddleName

Ha

Affiliation

Chemical Kinomics Research Center, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, Republic of Korea

Email

-

City

-

Orcid

-

Volume

45

Article Issue

1

Related Issue

34403

Issue Date

2022-06-01

Receive Date

2021-08-28

Publish Date

2022-06-01

Page Start

191

Page End

199

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 45_Issue 1_Pages 191-199.pdf

PDF . 899.7kB

Link

https://bpsa.journals.ekb.eg/article_239431.html

Detail API

https://bpsa.journals.ekb.eg/service?article_code=239431

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16

Type

Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

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

MainTitle

SYNTHESIS OF TWO NOVEL DERIVATIVES OF CYCLOSPORIN A AND EVALUATION OF THEIR ANTIPROLIFERATIVE EFFECT ON CANCER CELL LINES

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Article

Created At

22 Jan 2023